{"id":35318,"date":"2022-10-25T17:35:58","date_gmt":"2022-10-25T09:35:58","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=35318"},"modified":"2025-06-30T16:44:01","modified_gmt":"2025-06-30T08:44:01","slug":"%e3%80%90apexbioaapexbt-%e3%80%91chromatinepigenetics%e8%a1%a8%e8%a7%80%e9%81%ba%e5%82%b3%e5%ad%b8-apexbio%e5%8f%b0%e7%81%a3%e4%bb%a3%e7%90%86%e5%95%86","status":"publish","type":"post","link":"http:\/\/biopioneer.com.tw\/?p=35318","title":{"rendered":"\u3010APExBIO\/Aapexbt \u3011Chromatin\/Epigenetics\u8868\u89c0\u907a\u50b3\u5b78-APExBIO\u53f0\u7063\u4ee3\u7406\u5546"},"content":{"rendered":"<p><a href=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/APExBIO_logo.jpg\"><img decoding=\"async\" loading=\"lazy\" class=\"alignnone wp-image-34027 \" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/APExBIO_logo.jpg\" alt=\"APExBIO_logo\" width=\"290\" height=\"63\" srcset=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/APExBIO_logo.jpg 811w, http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/APExBIO_logo-300x65.jpg 300w\" sizes=\"(max-width: 290px) 100vw, 290px\" \/><\/a><\/p>\n<h2><span style=\"font-size: 12pt;\"><a href=\"http:\/\/www.apexbt.com\/\">APExBIO\u53f0\u7063\u4ee3\u7406\u5546<\/a><\/span><\/h2>\n<p>APExBIO\u63d0\u4f9b\u512a\u8cea\u7684\u80dc\u80bd\u548c\u751f\u7269\u5206\u6790\u8a66\u5291\uff0c\u5ee3\u6cdb\u7522\u54c1\u7dda\u5982Protease\u3001Chromatin\/Epigenetics\u8868\u89c0\u907a\u50b3\u5b78\u3001MAPK Signal\u3001DNA Damege\/DNA repair\u3001\u7d30\u80de\u51cb\u4ea1\u3001\u816b\u7624\u751f\u7269\u5b78\u3001Stem cell\u7b49\u7814\u7a76\u9818\u57df\uff0c \u9084\u63d0\u4f9b\u5b9a\u5236\u7684\u670d\u52d9\uff0c\u5305\u62ec\u591a\u80bd\u5408\u6210\uff0c\u6297\u9ad4\u7684\u751f\u7522\u548c\u6aa2\u6e2c\u7684\u767c\u5c55\u3002\u7522\u54c1\u7ddaDNA\/RNA prep kit\u3001Drug Screening panel\u3001Bioactive peptides\u3001Growth factors\u3001Biotinylation Reagents\u3001tag peptides\u3001amino Acids\u3001Growth factors\u7b49\u3002APExBIO\u7522\u54c1\u8cea\u91cf\u90fd\u4f34\u96a8\u8457\u8b49\u66f8\u7684\u5206\u6790\uff0c\u9ad8\u6548\u6db2\u76f8\u8272\u8b5c\uff0c\u8cea\u8b5c\uff0c\u548cHMNR\u6578\u64da\u3002APExBIO\u63d0\u4f9b\u4e00\u7cfb\u5217Chromatin\/Epigenetics\u8868\u89c0\u907a\u50b3\u5b78\u4e4b\u751f\u7269\u5316\u5408\u7269, \u5305\u62ec<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=33999\">MG 149 \u00a0(Tip60 HAT inhibitor) \u9078\u64c7\u6027\u6291\u5236\u5291<strong><u>\u00a0<\/u><\/strong><\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34002\">4&#8242;-bromo-Resveratrol<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34010\">MS023<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34348\">CHZ868<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35251\">Chidamide<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35254\">RGFP966<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35260\">EPZ-6438<\/a>\u3001<a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35291\">Bromodomain Inhibitor, (+)-JQ1<\/a>\u7b49\u7cfb\u5217\u5546\u54c1\u3002<\/p>\n<p>&nbsp;<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"https:\/\/www.apexbt.com\/media\/diy\/images\/pathway\/epigenetics.png\" alt=\"\" width=\"808\" height=\"562\" \/><\/p>\n<p>\u8868\u89c0\u907a\u50b3\u5b78(Epigenetics)\u662f\u57fa\u56e0\u8868\u9054\u7684\u53ef\u907a\u50b3\u4fee\u98fe(heritable modifications)\uff0c\u8207 DNA \u5e8f\u5217(DNA sequence)\u7684\u8b8a\u5316\u7121\u95dc\u3002\u8868\u89c0\u907a\u50b3\u4fee\u98fe(Epigenetic modifications)\u4e3b\u8981\u767c\u751f\u5728 DNA \u6216\u7d44\u86cb\u767d\u516b\u805a\u9ad4(histone octamer)\u4e0a\u3002\u6709\u5e7e\u7a2e\u985e\u578b\u7684\u8868\u89c0\u907a\u50b3\u5b78\u4fee\u98fe(epigenetics modifications)\uff0cDNA-\u7532\u57fa\u8f49\u79fb\u9176 (DNMT) \u7684 DNA \u7532\u57fa\u5316\u548c\u7d44\u86cb\u767d\u7684\u5171\u50f9\u4fee\u98fe\uff0c\u4f8b\u5982\u4e59\u91af\u5316(acetylation)\u3001\u7532\u57fa\u5316(methylation)\u3001\u78f7\u9178\u5316(phosphorylation)\u548c\u6cdb\u7d20\u5316(ubiquitination)\u3002\u7d44\u86cb\u767d\u4e59\u91af\u8f49\u79fb\u9176 (HAT) \u7684\u7d44\u86cb\u767d\u4e59\u91af\u5316\u53c3\u8207\u8f49\u9304\u6fc0\u6d3b\uff0c\u800c\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176 (HDAC) \u7684\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u8207\u8f49\u9304\u6291\u5236(transcriptional repression)\u6709\u95dc\u3002\u7d44\u86cb\u767d\u53bb\u7532\u57fa\u5316(Histone demethylation)\u8207\u8cf4\u6c28\u9178\u7279\u7570\u6027\u53bb\u7532\u57fa\u5316\u9176 (lysine-specific demethylase , LSD) \u548c\u542b\u6709\u7d44\u86cb\u767d\u53bb\u7532\u57fa\u5316\u9176 (JHDM) \u7684 JmjC \u7d50\u69cb\u57df(JmjC domain)\u6709\u95dc\u3002<\/p>\n<p>\u6838\u5c0f\u9ad4(nucleosome)\u7531\u56db\u7a2e\u7d44\u86cb\u767d\uff08H2A\u3001H2B\u3001H3 \u548c H4\uff09\u7d44\u6210\uff0c\u5b83\u5011\u662f\u67d3\u8272\u8cea(chromatin)\u7684\u4e3b\u8981\u7d44\u6210\u90e8\u5206\u3002\u7279\u5b9a\u5316\u5b78\u57fa\u5718\u7684\u6dfb\u52a0\u548c\u53bb\u9664\u7a31\u70ba\u8868\u89c0\u907a\u50b3\u6a19\u8a18(epigenetic marks)\uff0c\u5b83\u8abf\u7bc0\u67d3\u8272\u8cea\u7d50\u69cb\u4e26\u5f71\u97ff\u57fa\u56e0\u8868\u9054\u3002\u6b64\u5916\uff0cRNA \u8207\u6291\u5236\u6027\u67d3\u8272\u8cea\u72c0\u614b(repressive chromatin state)\u7684\u5f62\u6210\u5bc6\u5207\u76f8\u95dc\u3002<\/p>\n<p>\u8868\u89c0\u907a\u50b3(Epigenetic)\u6a5f\u5236\u5728\u7d30\u80de\u6c34\u5e73\u4e0a\u97ff\u61c9\u74b0\u5883\u8b8a\u5316\uff0c\u5f9e\u800c\u5f71\u97ff\u7d30\u80de\u53ef\u5851\u6027(plasticity)\u3002\u67d3\u8272\u8cea(Chromatin)\u548c\u8868\u89c0\u907a\u50b3\u8abf\u63a7(epigenetic regulation)\u5728\u767c\u80b2\u548c\u61c9\u6fc0\u53cd\u61c9\u671f\u9593\u7684\u57fa\u56e0\u7d44\u7de8\u7a0b\u4e2d\u767c\u63ee\u91cd\u8981\u4f5c\u7528\uff0c\u8868\u89c0\u907a\u50b3\u5b78\u7f3a\u9677(defects in epigenetics)\u53ef\u5c0e\u81f4\u764c\u75c7(cancer)\u3001\u708e\u75c7(inflammation)\u548c\u4ee3\u8b1d\u7d0a\u4e82(metabolic disorders)\u7b49\u3002MG 149 \u662f\u4e00\u7a2e\u7d44\u86cb\u767d\u4e59\u9170\u8f49\u79fb\u9176 (HAT) \u6291\u88fd\u5291\uff0c\u5c0d Tip60 \u548c MOF \u7684 IC50 \u503c\u5206\u5225\u70ba 74\u03bcM \u548c 47\u03bcM [1]\u3002<\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=33999\">MG 149 \u00a0(Tip60 HAT inhibitor) \u9078\u64c7\u6027\u6291\u5236\u5291<strong>\u00a0| CAS#<\/strong>\u00a0<strong>1243583-85-8 APExBIO<\/strong><strong>\u8ca8\u865f<\/strong>\u00a0B3276<\/a><\/span><\/p>\n<p>MG 149 \u662f\u6f06\u6a39\u9178\u884d\u751f\u7269(anacardic acid derivative)\u3002\u5b83\u986f\u793a\u5c0d MYST \u985e\u578b\u7684 HAT(histone acetyltransferases)\uff1aTip60 \u548c MOF \u7684\u9078\u64c7\u6027\u6291\u5236(selective inhibition)\uff0cIC50 \u503c\u5206\u5225\u70ba 74\u03bcM \u548c 47\u03bcM\u3002\u5c0d\u63a5\u7814\u7a76\u8868\u660e\uff0cMG 149 \u5c0d Tip60 \u7684\u6291\u5236\u4f5c\u7528\u76f8\u5c0d\u65bc Tip60 \u7684 Ac-CoA \u7d50\u5408\u53e3\u888b\u4e2d\u7684 Ac-CoA \u5177\u6709\u7af6\u722d\u6027\u3002 MG 149 \u9084\u4f7f\u7528\u751f\u7269\u7d20\u5316\u7d44\u86cb\u767d H3 \u6216\u7d44\u86cb\u767d H4 \u80bd\u4f5c\u70ba\u5e95\u7269\u6291\u5236 HeLa \u7d30\u80de\u6838\u63d0\u53d6\u7269\u4e2d HAT \u7684\u6d3b\u6027\u3002\u8207\u7d44\u86cb\u767d H4 \u76f8\u6bd4\uff0c\u5b83\u88ab\u767c\u73fe\u5c0d\u7d44\u86cb\u767d H3 \u66f4\u6709\u6548\u3002\u6b64\u5916\uff0cDNA \u5fae\u9663\u5217(DNA microarrays) , \u986f\u793a MG149 \u6291\u5236 p53 \u548c NF-kB \u901a\u8def\u4ee5\u53ca\u6578\u91cf\u975e\u5e38\u6709\u9650\u7684\u5176\u4ed6\u901a\u8def [1, 2]\u3002<\/p>\n<p><img decoding=\"async\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/09\/B3276_1-1.jpg\" alt=\"\" \/><\/p>\n<ul>\n<li>1. Zichong Li. &#8220;Functional characterization of transcription elongation machinery in HIV transcription and latency.&#8221; University of California. 2019.<\/li>\n<li>2. Li Z, Mbonye U, et al. &#8220;The KAT5-Acetyl-Histone4-Brd4 axis silences HIV-1 transcription and promotes viral latency.&#8221; PLoS Pathog. 2018 Apr 23;14(4):e1007012.\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/29684085\">PMID:29684085<\/a><\/li>\n<\/ul>\n<p><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=34002\">4&#8242;-bromo-Resveratrol (Sirt1 \u548c Sirt3 \u6291\u5236\u5291) | CAS# 1224713-90-9 APExBIO\u8ca8\u865f C3552<\/a><\/p>\n<p>4&#8242;-bromo-Resveratrol \u662f\u4e00\u7a2e Sirt1 \u548c Sirt3 \u6291\u5236\u5291\u3002Sirtuins \u662f\u8abf\u7bc0\u8870\u8001\u904e\u7a0b(aging processes)\u548c\u8a31\u591a\u751f\u7406\u529f\u80fd\u7684\u86cb\u767d\u8cea\u812b\u4e59\u91af\u9176(protein deacetylases)\u3002\u767d\u85dc\u8606\u9187\u53ef\u6fc0\u6d3b\u4eba\u985e Sirt1 \u4e26\u6291\u5236 Sirt3\uff0c\u4e26\u53ef\u4ee5\u6a21\u64ec\u5361\u8def\u91cc\u9650\u5236\u6548\u61c9(mimic calorie restriction)\uff0c\u5305\u62ec\u5728\u4f4e\u7b49\u751f\u7269\u4e2d\u5ef6\u9577\u58fd\u547d\u3002\u9ad4\u5916(In vitro)\uff1a\u5728\u5148\u524d\u7684\u7814\u7a76\u4e2d\u4f7f\u7528 4&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u7814\u7a76\u4e86\u53bb\u4e59\u9170\u5316\u9176\u8abf\u7bc0\u3002 \u00a04&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u6291\u5236 Sirt3 \u7684\u6548\u529b\u6bd4\u767d\u85dc\u8606\u9187\u9ad8\u5f97\u591a\uff0c\u800c\u4e14\u5b83\u9084\u6291\u5236\u800c\u4e0d\u662f\u6fc0\u6d3b Sirt1\u3002\u4eba Sirt3\/4&#8242;-\u6eb4\u767d\u85dc\u8606\u9187\u80bd\u8907\u5408\u7269\u7684\u6676\u9ad4\u7d50\u69cb\u78ba\u5b9a\u4e86\u5169\u500b\u7d50\u5408\u4f4d\u9ede\u3002\u5167\u90e8\u4f4d\u9ede\u5f15\u8d77\u4e86\u6709\u6548\u7684\u6291\u5236\u4f5c\u7528\u3002 \u00a04&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u5e72\u64fe NAD+ \u548c\u5e95\u7269\u80bd\u7684\u7d50\u5408\uff0c\u4e26\u5c07\u5176\u6eb4-\u82ef\u57fa\u57fa\u5718\u5ef6\u4f38\u5230\u7121\u6cd5\u8b58\u5225\u7684\u4f4d\u9ede\u53e3\u888b\u4e2d\u3002\u767c\u73fe \u00a04&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u7684\u7b2c\u4e8c\u500b\u7d50\u5408\u4f4d\u9ede\u4f4d\u65bc Sirt3 \u7684\u8868\u9762\uff0c\u4e26\u901a\u904e\u5169\u500b\u87ba\u65cb\u9023\u63a5\u5230\u80bd\u7d50\u5408\u6d3b\u6027\u4f4d\u9ede\u74b0\u3002\u5728 Sirt1 \u4e2d\uff0c\u8a72\u4f4d\u9ede\u4f3c\u4e4e\u5305\u542b\u4e00\u500b\u5c0d\u5176\u88ab\u5c0f\u5206\u5b50\u6fc0\u6d3b\u81f3\u95dc\u91cd\u8981\u7684\u6b98\u57fa\uff0c\u56e0\u6b644&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u69cb\u6210\u4e86\u9577\u671f\u5c0b\u627e\u7684\u8b8a\u69cb Sirt1 \u6fc0\u6d3b\u5291\u7d50\u5408\u4f4d\u9ede\u7684\u5019\u9078\u8005(candidate) [1]\u3002<strong>\u9ad4\u5167(In vivo)\uff1a<\/strong>\u5230\u76ee\u524d\u70ba\u6b62\uff0c\u9084\u6c92\u6709 4&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u7684\u52d5\u7269\u9ad4\u5167\u6578\u64da\u3002<strong>\u81e8\u5e8a\u8a66\u9a57\uff1a<\/strong>\u622a\u81f3\u76ee\u524d\uff0c4&#8242;-\u6eb4\u767d\u85dc\u8606\u9187(4\u2019-bromo-Resveratrol)\u4ecd\u8655\u65bc\u81e8\u5e8a\u524d\u958b\u767c\u968e\u6bb5(preclinical development stage)\u3002<\/p>\n<p><img decoding=\"async\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/c3552-CAS-1224713-90-9-300x282.png\" alt=\"c3552 CAS-1224713-90-9\" \/><\/p>\n<ul>\n<li>1. Wang LJ, Lee YC, et al. &#8220;Non-mitotic effect of albendazole triggers apoptosis of human leukemia cells via SIRT3\/ROS\/p38 MAPK\/TTP axis-mediated TNF-\u03b1 upregulation.&#8221; Biochem Pharmacol. 2018 Nov 7. pii: S0006-2952(18)30472-6.\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/30414389\">PMID:30414389<\/a><\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=34010\">MS023 (type I PRMTs inhibitor\u6291\u5236\u5291) | CAS# 1831110-54-3APExBIO\u8ca8\u865f B6183<\/a><\/span><\/p>\n<p>&nbsp;<\/p>\n<p>MS023 is a type I PRMTs inhibitor.Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. PRMT overexpression has been observed in a variety of human diseases including cancer. PRMTs has been divided into three categories: type I PRMTs for catalyzing mono- and asymmetric dimethylation of arginine residues, type II PRMTs for catalyzing mono- and symmetric dimethylation of arginine residues, and type III PRMT for catalyzing only monomethylation of arginine residues.<\/p>\n<p><img decoding=\"async\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/2022\/09\/MS023-type-I-PRMTs-inhibitor%E6%8A%91%E5%88%B6%E5%8A%91-CAS-1831110-54-3APExBIO%E8%B2%A8%E8%99%9F-B6183-300x300.png\" alt=\"MS023 (type I PRMTs inhibitor\u6291\u5236\u5291) CAS# 1831110-54-3APExBIO\u8ca8\u865f B6183\" \/><\/p>\n<p>MS023 \u662f\u4e00\u7a2e I \u578b PRMTs \u6291\u5236\u5291\u3002\u86cb\u767d\u8cea\u7cbe\u6c28\u9178\u7532\u57fa\u8f49\u79fb\u9176 (inhibitor.Protein arginine methyltransferases ,PRMT) \u5728\u5404\u7a2e\u751f\u7269\u904e\u7a0b\u4e2d\u767c\u63ee\u8457\u95dc\u9375\u4f5c\u7528\u3002\u5df2\u5728\u5305\u62ec\u764c\u75c7(cancer)\u5728\u5167\u7684\u591a\u7a2e\u4eba\u985e\u75be\u75c5\u4e2d\u89c0\u5bdf\u5230 PRMT \u904e\u5ea6\u8868\u9054(overexpression)\u3002 PRMTs\u5206\u70ba\u4e09\u985e\uff1aI\u578bPRMTs\u7528\u65bc\u50ac\u5316\u7cbe\u6c28\u9178\u6b98\u57fa(arginine residues)\u7684\u55ae\u7532\u57fa\u5316\u548c\u4e0d\u5c0d\u7a31\u4e8c\u7532\u57fa\u5316\uff0cII\u578bPRMTs\u7528\u65bc\u50ac\u5316\u7cbe\u6c28\u9178\u6b98\u57fa(arginine residues)\u7684\u55ae\u7532\u57fa\u5316\u548c\u5c0d\u7a31\u4e8c\u7532\u57fa\u5316(symmetric demethylation)\uff0cIII\u578bPRMTs\u50c5\u50ac\u5316\u7cbe\u6c28\u9178\u6b98\u57fa\u7684\u55ae\u7532\u57fa\u5316(monomethylation)\u3002\u9ad4\u5916(In vitro)\uff1a\u5148\u524d\u7684\u7814\u7a76\u8868\u660e\uff0cMS023 \u5c0d I \u578b PRMT \u5177\u6709\u51fa\u8272\u7684\u6548\u529b\uff0c\u4f46\u5c0d II \u578b\u548c III \u578b PRMT\u3001\u86cb\u767d\u8cea\u8cf4\u6c28\u9178\u7532\u57fa\u8f49\u79fb\u9176(protein lysine methyltransferases)\u4ee5\u53ca DNA \u7532\u57fa\u8f49\u79fb\u9176(DNA methyltransferases)\u5747\u5b8c\u5168\u7121\u6d3b\u6027\u3002\u6b64\u5916\uff0cPRMT6 \u8207 MS023 \u7684\u6676\u9ad4\u7d50\u69cb\u8868\u660e MS023 \u8207\u5e95\u7269\u7d50\u5408\u4f4d\u9ede\u7d50\u5408\u3002\u6b64\u5916\uff0cMS023 \u53ef\u4ee5\u6709\u6548\u964d\u4f4e\u7d44\u86cb\u767d\u7cbe\u6c28\u9178\u4e0d\u5c0d\u7a31\u4e8c\u7532\u57fa\u5316\u7684\u7d30\u80de\u6c34\u5e73\u3002\u6b64\u5916\uff0cMS023 \u53ef\u4ee5\u964d\u4f4e\u7cbe\u6c28\u9178\u4e0d\u5c0d\u7a31\u4e8c\u7532\u57fa\u5316\u7684\u6c34\u5e73\uff0c\u540c\u6642\u9084\u53ef\u4ee5\u589e\u52a0\u7cbe\u6c28\u9178\u55ae\u7532\u57fa\u5316\u548c\u5c0d\u7a31\u4e8c\u7532\u57fa\u5316\u7684\u7d30\u80de\u6c34\u5e73 [1]\u3002\u9ad4\u5167\uff1a\u5230\u76ee\u524d\u70ba\u6b62\uff0c\u9084\u6c92\u6709\u52d5\u7269\u9ad4\u5167\u6578\u64da\u5831\u5c0e\u3002\u81e8\u5e8a\u8a66\u9a57\uff1a\u622a\u81f3\u76ee\u524d\uff0cMS023\u4ecd\u8655\u65bc\u81e8\u5e8a\u524d\u958b\u767c\u968e\u6bb5\u3002<\/p>\n<ul>\n<li>1. Pyun JH, Kim HJ, et al. &#8220;Cardiac specific PRMT1 ablation causes heart failure through CaMKII dysregulation.&#8221; Nat Commun. 2018 Nov 30;9(1):5107.\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/30504773\">PMID:30504773<\/a><\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=34348\">CHZ868 | APExBIO\u00a0 \u8ca8\u865fB5980<\/a>\u00a0<\/span>Type II JAK2 inhibitor<\/p>\n<p>&nbsp;<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/09\/CHZ868-APExBIO-%E8%B2%A8%E8%99%9FB5980-1.png\" alt=\"\" width=\"402\" height=\"315\" \/><\/p>\n<p>CHZ868 \u662f\u4e00\u7a2e II \u578b JAK2 \u6291\u5236\u5291\uff0cIC50 \u503c\u70ba 110 nM [1]\u3002JAK2\uff08Janus \u6fc0\u9176 2\uff09\u662f\u4e00\u7a2e\u975e\u53d7\u9ad4\u916a\u6c28\u9178\u6fc0\u9176(non-receptor tyrosine kinase)\u3002 JAK2 \u7684\u7a81\u8b8a\u8207\u8a31\u591a\u9aa8\u9ad3\u589e\u751f\u6027(myeloproliferative disorders)\u75be\u75c5\u6709\u95dc\u3002\u5728 CRLF2 \u91cd\u6392\u7684\u4eba B-ALL \u7d30\u80de MHH-CALL4 \u4e2d\uff0cCHZ868 \u6709\u6548\u6291\u5236 JAK2 \u78f7\u9178\u5316\u548c\u7d30\u80de\u751f\u9577 [1]\u3002 CHZ868 \u662f\u4e00\u7a2e II \u578b JAK2 \u6291\u5236\u5291\u3002\u5728 JAK2V617F SET2 \u7d30\u80de\u4e2d\uff0cCHZ868 \u6709\u6548\u6291\u5236\u7d44\u6210\u578b JAK2 \u548c STAT5 \u78f7\u9178\u5316\uff0c\u4e26\u6291\u5236\u7d30\u80de\u589e\u6b96\uff0cGI50 \u503c\u70ba 59 nM\u3002\u5728 MPLW515L \u7a81\u8b8a\u7d30\u80de\u4e2d\uff0cCHZ868 \u6709\u6548\u6291\u5236\u7d30\u80de\u589e\u6b96\u4e26\u6d88\u9664 JAK2 \u6fc0\u6d3b\u74b0\u4e2d Y1007\/Y1008 \u7684\u78f7\u9178\u5316\u3002\u5728 I \u578b JAK \u6291\u5236\u5291\u6301\u4e45\u6027\u7d30\u80de\u4e2d\uff0cCHZ868 \u6709\u6548\u4e14\u6fc3\u5ea6\u4f9d\u8cf4\u6027\u5730\u6291\u5236 JAK2 \u78f7\u9178\u5316\u548c JAK2V617F \u6216 MPLW515L \u7d30\u80de\u7684\u589e\u6b96(cell proliferation) [2]\u3002\u5728\u60a3\u6709\u4eba\u985e\u6216\u9f20 B-ALL \u7684\u5c0f\u9f20\u4e2d\uff0cCHZ868 \u63d0\u9ad8\u4e86\u5b58\u6d3b\u7387\u3002\u5728 JAK2 \u4f9d\u8cf4\u6027 B-ALL \u5c0f\u9f20\u4e2d\uff0c\u8207\u55ae\u7368\u4f7f\u7528 CHZ868 \u76f8\u6bd4\uff0cCHZ868 \u548c\u5730\u585e\u7c73\u677e(dexamethasone)\u5354\u540c\u8a98\u5c0e\u7d30\u80de\u51cb\u4ea1\u4e26\u63d0\u9ad8\u5b58\u6d3b\u7387 [1]\u3002\u5728 Jak2V617F \u9a45\u52d5\u7684\u7d05\u7d30\u80de\u589e\u591a\u75c7 (polycythemiavera , PV) \u4e2d\uff0cCHZ868\uff0830 &#8211; 40 mg\/kg \u53e3\u670d\uff0c\u6bcf\u5929\u4e00\u6b21\uff09\u6291\u5236 JAK-STAT \u4fe1\u865f\u50b3\u5c0e\u4e26\u986f\u8457\u964d\u4f4e\u9aa8\u9ad3\u4e2d\u7a81\u8b8a\u7d30\u80de\u7684\u6bd4\u4f8b\u3002\u5728 MPLW515L \u8a98\u5c0e\u7684\u9aa8\u9ad3\u7e96\u7dad\u5316 (MF) \u4e2d\uff0cCHZ868 \u5b8c\u5168\u6291\u5236 STAT3 \u548c STAT5 \u78f7\u9178\u5316\uff0c\u4e26\u964d\u4f4e JAK2 \u78f7\u9178\u5316\u3002 CHZ868 \u9084\u4ee5\u5291\u91cf\u4f9d\u8cf4\u7684\u65b9\u5f0f\u63d0\u9ad8\u4e86\u751f\u5b58\u7387\u4e26\u6e1b\u5c11\u4e86\u809d\u816b\u5927(hepatomegaly) [2]\u3002<\/p>\n<p><img decoding=\"async\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/09\/CHZ868-APExBIO-%E8%B2%A8%E8%99%9FB5980.jpg\" alt=\"\" \/><\/p>\n<ol>\n<li>Tvorogov D, Thomas D, et al. &#8220;Accumulation of JAK activation loop phosphorylation is linked to type I JAK inhibitor withdrawal syndrome in myelofibrosis.&#8221; Sci Adv. 2018 Nov 28;4(11):eaat3834.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/30498775\">PMID:30498775<\/a><\/li>\n<\/ol>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=35251\">Chidamide | CAS#743420-02-2APExBIO\u00a0 \u8ca8\u865fB5916<\/a><\/span><\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/1-Chidamide-CAS743420-02-2APExBIO-%E8%B2%A8%E8%99%9FB5916.png\" alt=\"\" width=\"298\" height=\"233\" \/><\/p>\n<p>Product Citation+1<\/p>\n<p>Novel HDAC inhibitor<\/p>\n<p>Chidamide \u662f\u4e00\u7a2e\u65b0\u578b\u82ef\u7532\u9170\u80fa\u578b\u7d44\u86cb\u767d\u812b\u4e59\u91af\u9176 (benzamide-type histone deacetylase , HDAC) \u6291\u5236\u5291\u3002\u4eba\u5011\u7814\u7a76\u4e86 CS055 \u5c0d\u4eba\u767d\u8840\u75c5\u7d30\u80de\u7cfb\u548c\u539f\u767c\u6027\u9aa8\u9ad3\u6027\u767d\u8840\u75c5\u7d30\u80de\u589e\u6b96(proliferation)\u3001\u5206\u5316(differentiation)\u548c\u51cb\u4ea1(apoptosis)\u7684\u5f71\u97ff\u3002\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176 (Histone deacetylases , HDAC) \u662f\u4e00\u7cfb\u5217\u9176\uff0c\u5176\u4f5c\u7528\u662f\u4f7f\u7d44\u86cb\u767d\u7684\u6c28\u57fa\u672b\u7aef\u8cf4\u6c28\u9178\u6b98\u57fa(amino-terminal lysine residues)\u4e59\u91af\u5316\u548c\u53bb\u4e59\u91af\u5316\uff0c\u5f9e\u800c\u5c0e\u81f4\u67d3\u8272\u8cea\u7d50\u69cb\u7684\u91cd\u5851(remodeling)\u4e26\u5f71\u97ff\u67d3\u8272\u8cea(chromatin)\u5c0d\u8f49\u9304\u56e0\u5b50\u7684\u53ef\u53ca\u6027\uff0c\u5f9e\u800c\u555f\u52d5\u57fa\u56e0\u8f49\u9304(gene transcription)\u3002 [2 ]\u897f\u9054\u672c\u80fa(Chidamide) \u5c0d\u7d30\u80de\u9031\u671f(cell cycle)\u6709\u5f71\u97ff\uff0c\u5b83\u986f\u8457\u964d\u4f4e\u4e86\u4e0d\u540c p53 \u72c0\u614b\u7684 BEL-7402 \u548c HCC-9204 \u7d30\u80de\u7684 S \u671f\u7d30\u80de\u5206\u6578\uff0c\u540c\u6642\u8a98\u5c0e G1 \u671f\u7d30\u80de\u5206\u6578\u986f\u8457\u589e\u52a0\u3002\u96a8\u8457\u5291\u91cf\u7684\u589e\u52a0\uff0c\u897f\u9054\u672c\u80fa(Chidamide)\u986f\u8457\u6539\u8b8a\u4e86\u968e\u6bb5\u5206\u6578\u4e2d\u7684\u7d30\u80de\u6578\u91cf\u3002 [2]\u672c\u7814\u7a76\u7d50\u679c\u8868\u660e\uff0c\u897f\u9054\u672c\u80fa(Chidamide)\u662f\u4e00\u7a2e HDACi\uff0c\u901a\u904e\u6291\u5236\u7d30\u80de\u589e\u6b96(cell proliferation)\u3001\u8a98\u5c0e\u4eba\u9ad4\u7d30\u80de\u5206\u5316(differentiation)\u548c\u51cb\u4ea1(apoptosis)\uff0c\u5728\u591a\u7a2e\u8840\u6db2\u7cfb\u7d71\u60e1\u6027\u816b\u7624(haematological malignancies)\u4e2d\u5177\u6709\u6f5b\u5728\u7684\u6cbb\u7642\u50f9\u503c\u3002<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/2ChidamideCAS743420-02-2APExBIO-%E8%B2%A8%E8%99%9FB5916.jpg\" alt=\"\" width=\"490\" height=\"353\" \/><\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=35254\">RGFP966 | CAS#1357389-11-7\/1396841-57-8 APExBIO\u00a0 \u8ca8\u865fA8803<\/a><\/span><\/p>\n<p>Product Citation+4<\/p>\n<p>Specific HDAC3 inhibitor<\/p>\n<p>Chidamide \u662f\u4e00\u7a2e\u65b0\u578b\u82ef\u7532\u91af\u80fa\u578b\u7d44\u86cb\u767d\u812b\u4e59\u91af\u9176 (benzamide-type histone deacetylase , HDAC) \u6291\u5236\u5291\u3002\u4eba\u5011\u7814\u7a76\u4e86 CS055 \u5c0d\u4eba\u767d\u8840\u75c5\u7d30\u80de\u7cfb\u548c\u539f\u767c\u6027\u9aa8\u9ad3\u6027\u767d\u8840\u75c5\u7d30\u80de\u589e\u6b96(proliferation)\u3001\u5206\u5316(differentiation)\u548c\u51cb\u4ea1(apoptosis)\u7684\u5f71\u97ff\u3002\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176 (Histone deacetylases , HDAC) \u662f\u4e00\u7cfb\u5217\u9176\uff0c\u5176\u4f5c\u7528\u662f\u4f7f\u7d44\u86cb\u767d\u7684\u6c28\u57fa\u672b\u7aef\u8cf4\u6c28\u9178\u6b98\u57fa(amino-terminal lysine residues)\u4e59\u91af\u5316\u548c\u53bb\u4e59\u91af\u5316\uff0c\u5f9e\u800c\u5c0e\u81f4\u67d3\u8272\u8cea\u7d50\u69cb\u7684\u91cd\u5851(remodeling)\u4e26\u5f71\u97ff\u67d3\u8272\u8cea(chromatin)\u5c0d\u8f49\u9304\u56e0\u5b50\u7684\u53ef\u53ca\u6027\uff0c\u5f9e\u800c\u555f\u52d5\u57fa\u56e0\u8f49\u9304(gene transcription)\u3002 [2 ]\u897f\u9054\u672c\u80fa(Chidamide) \u5c0d\u7d30\u80de\u9031\u671f(cell cycle)\u6709\u5f71\u97ff\uff0c\u5b83\u986f\u8457\u964d\u4f4e\u4e86\u4e0d\u540c p53 \u72c0\u614b\u7684 BEL-7402 \u548c HCC-9204 \u7d30\u80de\u7684 S \u671f\u7d30\u80de\u5206\u6578\uff0c\u540c\u6642\u8a98\u5c0e G1 \u671f\u7d30\u80de\u5206\u6578\u986f\u8457\u589e\u52a0\u3002\u96a8\u8457\u5291\u91cf\u7684\u589e\u52a0\uff0c\u897f\u9054\u672c\u80fa(Chidamide)\u986f\u8457\u6539\u8b8a\u4e86\u968e\u6bb5\u5206\u6578\u4e2d\u7684\u7d30\u80de\u6578\u91cf\u3002 [2]\u672c\u7814\u7a76\u7d50\u679c\u8868\u660e\uff0c\u897f\u9054\u672c\u80fa(Chidamide)\u662f\u4e00\u7a2e HDACi\uff0c\u901a\u904e\u6291\u5236\u7d30\u80de\u589e\u6b96(cell proliferation)\u3001\u8a98\u5c0e\u4eba\u9ad4\u7d30\u80de\u5206\u5316(differentiation)\u548c\u51cb\u4ea1(apoptosis)\uff0c\u5728\u591a\u7a2e\u8840\u6db2\u7cfb\u7d71\u60e1\u6027\u816b\u7624(haematological malignancies)\u4e2d\u5177\u6709\u6f5b\u5728\u7684\u6cbb\u7642\u50f9\u503c\u3002<\/p>\n<p><a>1. Zhang M, Urabe G, et al. &#8220;HDAC6 Regulates the MRTF-A\/SRF Axis and Vascular Smooth Muscle Cell Plasticity.&#8221; JACC Basic Transl Sci. 2018 Dec 31;3(6):782-795.<\/a>\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/30623138\" target=\"_blank\" rel=\"noopener\">PMID:30623138<\/a><\/p>\n<p><a>2. Huang L, Lai WH, et al. &#8220;Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor.&#8221; ACS Med Chem Lett. 2018 Feb 6;9(3):268-273.<\/a>\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/29541372\" target=\"_blank\" rel=\"noopener\">PMID:2954137<\/a><\/p>\n<p><a>3. Topper MJ, Vaz M, et al. &#8220;Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer.&#8221; Cell. 2017 Nov 30;171(6):1284-1300.e21.<\/a>\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/29195073\" target=\"_blank\" rel=\"noopener\">PMID:29195073<\/a><\/p>\n<p><a>4. Sun XY, Qu Y, et al. &#8220;Novel histone deacetylase inhibitor N25 exerts anti-tumor effects and induces autophagy in human glioma cells by inhibiting HDAC3.&#8221;Oncotarget. 2017 Sep 8;8(43):75232-75242.<\/a>\u00a0<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/29088860\" target=\"_blank\" rel=\"noopener\">PMID:29088860<\/a><\/p>\n<p>&nbsp;<\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=35260\">EPZ-6438 | CAS#1403254-99-8 APExBIO\u00a0 \u8ca8\u865fA8221<\/a><\/span><\/p>\n<p>EZH2 inhibitor, potent and selective<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/2-EPZ-6438-CAS1403254-99-8-APExBIO-%E8%B2%A8%E8%99%9FA8221.jpg\" alt=\"\" width=\"811\" height=\"563\" \/><\/p>\n<p>EPZ-6438 \u662f\u4e00\u7a2e\u6709\u6548\u4e14\u5177\u6709\u751f\u7269\u6d3b\u6027\u7684 EZH2 \u6291\u5236\u5291\uff0cEZH2 \u662f\u591a\u68b3\u6291\u5236\u8907\u5408\u7269 2 (polycomb repressive complex 2 , PRC2) \u7684\u50ac\u5316\u4e9e\u57fa\uff0c\u53ef\u50ac\u5316\u7d44\u86cb\u767d H3 (H3K27) \u7684\u8cf4\u6c28\u9178 27 \u7684\u7532\u57fa\u5316\uff0c\u5f9e\u800c\u6291\u5236\u542b\u6709\u4eba PRC2 \u7684\u91ce\u751f\u578b\u7684\u6d3b\u6027EZH2 \u7684\u6291\u5236\u5e38\u6578 Ki \u503c\u70ba 2.5 nM\u3002 EPZ-6438 \u7af6\u722d\u6027\u7d50\u5408 EZH2 \u7684 S-\u817a\u82f7\u7532\u786b\u6c28\u9178 (S-adenosylmethionine , SAM) \u7d50\u5408\u4f4d\u9ede\uff0c\u4e5f\u975e\u7af6\u722d\u6027\u7d50\u5408\u80bd\u6216\u6838\u5c0f\u9ad4\u5e95\u7269\u7684\u7d50\u5408\u4f4d\u9ede\u3002 EPZ-6438 \u9078\u64c7\u6027\u6291\u5236 EZH2\uff0c\u9078\u64c7\u6027\u6bd4 EZH1 \u9ad8 35 \u500d\u3002\u7814\u7a76\u7d50\u679c\u8868\u660e\uff0c\u901a\u904e EPZ-6438 \u4ecb\u5c0e\u7684 EZH2 \u6291\u5236\u5c0d\u5e7e\u7a2e\u764c\u75c7\u9014\u5f91\u7684\u5354\u540c\u4f5c\u7528\uff0cEPZ-6438 \u5728 MRT \u6a21\u578b\u4e2d\u8868\u73fe\u51fa\u986f\u8457\u4e14\u6301\u4e45\u7684\u6297\u816b\u7624\u6d3b\u6027\u3002<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/1-EPZ-6438-CAS1403254-99-8-APExBIO-%E8%B2%A8%E8%99%9FA8221.jpg\" alt=\"\" width=\"571\" height=\"436\" \/><\/p>\n<p><span style=\"color: #00ccff;\"><a style=\"color: #00ccff;\" href=\"http:\/\/biopioneer.com.tw\/?p=35291\">Bromodomain Inhibitor, (+)-JQ1 | CAS# 1268524-70-4 \u00a0APExBIO\u00a0 \u8ca8\u865fA1910<\/a><\/span><\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/2-Bromodomain-Inhibitor-JQ1-CAS-1268524-70-4-APExBIO-%E8%B2%A8%E8%99%9FA1910.jpg\" alt=\"\" width=\"550\" height=\"462\" \/><\/p>\n<p>BET bromodomain inhibitor<\/p>\n<p>Bromodomain Inhibitor, (+)-JQ1 \u662f\u4e00\u7a2e\u6709\u6548\u4e14\u9ad8\u5ea6\u7279\u7570\u6027\u7684 BET\uff08bromodomain and extra-terminal, \u6eb4\u7d50\u69cb\u57df\u548c\u672b\u7aef\u5916\uff09\u5bb6\u65cf\u7684\u6eb4\u7d50\u69cb\u57df\u6291\u5236\u5291\u3002 (+)-JQ1 \u8207 BRD4 \u6eb4\u7d50\u69cb\u57df 1 \u548c 2 \u7d50\u5408\uff0cKd \u503c\u5206\u5225\u70ba ~ 50 \u548c 90 nM\u3002\u8a72\u7d50\u5408\u8207\u4e59\u91af\u8cf4\u6c28\u9178(acetyl lysine)\u7af6\u722d\u3002 (+)-JQ1 \u53ef\u4ee5\u4f5c\u70ba\u4e00\u7a2e\u6709\u7528\u7684\u5316\u5b78\u63a2\u91dd\u4f86\u7814\u7a76 BET \u6eb4\u7d50\u69cb\u57df\u5728\u816b\u7624\u767c\u751f\u7684\u8f49\u9304\u8abf\u63a7\u4e2d\u7684\u4f5c\u7528\u3002JQ1 \u5c0d BRDT \u8868\u73fe\u51fa\u5f37\u70c8\u7684\u5291\u91cf\u548c\u6642\u9593\u4f9d\u8cf4\u6027\u6291\u5236\u4f5c\u7528\uff0c\u4e26\u4e14\u53ef\u4ee5\u986f\u8457\u964d\u4f4e BRDT \u7d50\u69cb\u8fd1\u89aa\u7684\u6d3b\u6027\u3002\u4ed4\u7d30\u89c0\u5bdf JQ1 \u7d50\u5408\u7684 BRDT \u8b49\u5be6 BRDT \u7684\u4e59\u91af\u8cf4\u6c28\u9178\u8b58\u5225\u4f4d\u9ede\u88ab\u963b\u65b7\u3002 [1]JQ1 \u4e0d\u7522\u751f\u93ae\u975c\u6216\u6297\u7126\u616e\u4f5c\u7528\uff0c\u800c\u662f\u4e00\u7a2e\u6709\u6548\u4e14\u9078\u64c7\u6027\u7684\u6eb4\u7d50\u69cb\u57df\u777e\u4e38\u7279\u7570\u6027\u86cb\u767d BRDT [2] \u6291\u5236\u5291\uff0c\u8a72\u86cb\u767d\u5c0d\u7cbe\u5b50\u767c\u751f\u904e\u7a0b\u4e2d\u7684\u67d3\u8272\u8cea\u91cd\u5851\u81f3\u95dc\u91cd\u8981\u3002\u901a\u904e\u963b\u65b7 BRDT\uff0cJQ1 \u6709\u6548\u5730\u963b\u65b7\u4e86\u777e\u4e38\u4e2d\u7cbe\u5b50\u7684\u7522\u751f\uff0c\u5f9e\u800c\u7522\u751f\u4e86\u6709\u6548\u7684\u907f\u5b55\u6548\u679c\uff0c\u800c\u6c92\u6709\u8207\u5148\u524d\u7814\u7a76\u7684\u7537\u6027\u6fc0\u7d20\u907f\u5b55\u85e5\u76f8\u95dc\u7684\u8ca0\u9762\u526f\u4f5c\u7528\u3002<\/p>\n<p><img decoding=\"async\" loading=\"lazy\" class=\"\" src=\"http:\/\/biopioneer.com.tw\/wp-content\/uploads\/downloads\/2022\/10\/1-Bromodomain-Inhibitor-JQ1-CAS-1268524-70-4-APExBIO-%E8%B2%A8%E8%99%9FA1910.jpg\" alt=\"\" width=\"573\" height=\"426\" \/><\/p>\n<p>Product Citation+6<\/p>\n<ol>\n<li>Amjad Ali, Jasmin Shafarin, et al. &#8220;Co-targeting BET bromodomain BRD4 and RAC1 suppresses growth, stemness and tumorigenesis by disrupting the c-MYC-G9a-FTH1axis and downregulating HDAC1 in molecular subtypes of breast cancer.&#8221; Int J Biol Sci. 2021 Oct 25;17(15):4474-4492.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/34803511\">PMID:34803511<\/a><\/li>\n<li>Victor Cy Mak, Xinran Li, et al. &#8220;p85\u03b2 alters response to EGFR inhibitor in ovarian cancer through p38 MAPK-mediated regulation of DNA repair.&#8221; Neoplasia. 2021 Jul;23(7):718-730.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/34144267\">PMID:34144267<\/a><\/li>\n<li>Lars Pache, Matthew D. Marsden, et al. &#8220;Pharmacological Activation of Non-canonical NF-\u03baB Signaling Activates Latent HIV-1 Reservoirs In Vivo.&#8221; Cell Rep Med. 2020 Jun 23;1(3):100037.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/33205060\">PMID:33205060<\/a><\/li>\n<li>Niklas Remke, Savita Bisht, et al. &#8220;Selective BET-bromodomain inhibition by JQ1 suppresses dendritic cell maturation and antigen-specific T-cell responses.&#8221; Cancer Immunol Immunother. 2020 Jul 10.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/32651619\">PMID:32651619<\/a><\/li>\n<li>Xiang Y, Tanaka Y, et al. &#8220;Dysregulation of BRD4 Function Underlies the Functional Abnormalities of MeCP2 Mutant Neurons.&#8221; Mol Cell. 2020;79(1):84-98.e9.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/32526163\">PMID:32526163<\/a><\/li>\n<li>Wu SY, Lee CF, et al. &#8220;Opposing Functions of BRD4 Isoforms in Breast Cancer.&#8221; Mol Cell. 2020;78(6):1114-1132.e10.<a href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/32446320\">PMID:32446320<\/a><\/li>\n<\/ol>\n<table width=\"553\">\n<tbody>\n<tr>\n<td width=\"139\">\u54c1\u9805<\/td>\n<td width=\"139\">CAS#<\/td>\n<td width=\"138\">#\u8ca8\u865f<\/td>\n<td width=\"138\">\u61c9\u7528<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34128\">Romidepsin (FK228, depsipeptide)<\/a><\/td>\n<td width=\"139\">\n<p>CAS#128517-07-7<\/p>\n<p>&nbsp;<\/td>\n<td width=\"138\">\u8ca8\u865fA8173<\/td>\n<td width=\"138\">HDAC1\/HDAC2\uff0c\u5f37\u6548\u548c\u9078\u64c7\u6027\u6291\u5236\u5291<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34607\">Pirarubicin<\/a><\/td>\n<td width=\"139\">CAS#72496-41-4<\/td>\n<td width=\"138\">\u8ca8\u865fB2295<\/td>\n<td width=\"138\">\u00a0anthracycline anti-neoplastic doxorubicin<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34599\">Tunicamycin<\/a><\/td>\n<td width=\"139\">CAS# 15663-27-1<\/td>\n<td width=\"138\">\n<p>\u8ca8\u865fA8321<\/p>\n<p>&nbsp;<\/td>\n<td width=\"138\">\u9ad8\u6548\u3001\u5ee3\u8b5c\u7684\u5316\u7642\u85e5\u7269<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34612\">Azithromycin<\/a><\/td>\n<td width=\"139\">CAS#83905-01-5<\/td>\n<td width=\"138\">\u00a0\u8ca8\u865fA2213<\/td>\n<td width=\"138\">Hsp90 inhibitor<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34765\">Bleomycin Sulfate<\/a><\/td>\n<td width=\"139\">\n<p>CAS# 9041-93-4<\/p>\n<p>&nbsp;<\/td>\n<td width=\"138\">\u8ca8\u865fB1398<\/td>\n<td width=\"138\">Antibiotic by inhibiting protein synthesis<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34625\">Nystatin (Fungicidin)<\/a><\/td>\n<td width=\"139\">CAS#1400-61-9<\/td>\n<td width=\"138\">\u8ca8\u865fB1993<\/td>\n<td width=\"138\">antifungal antibiotic<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34118\">Rapamycin<\/a><\/td>\n<td width=\"139\">CAS#53123-88-9<\/td>\n<td width=\"138\">\u8ca8\u865fA8167<\/td>\n<td width=\"138\">Original antifungal antibiotic<\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><a href=\"http:\/\/biopioneer.com.tw\/?p=34140\">Daptomycin<\/a><\/td>\n<td width=\"139\">CAS#103060-53-3<\/td>\n<td width=\"138\">\u8ca8\u865fA1206<\/td>\n<td width=\"138\">Calcium-dependent antibiotic<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<p>&nbsp;<\/p>\n<table width=\"553\">\n<tbody>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\">\u54c1\u9805<\/span><\/td>\n<td width=\"139\"><span style=\"color: #008080;\">CAS#<\/span><\/td>\n<td width=\"138\"><span style=\"color: #008080;\">#\u8ca8\u865f<\/span><\/td>\n<td width=\"138\"><span style=\"color: #008080;\">\u61c9\u7528<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=33999\">MG 149 \u00a0(Tip60 HAT inhibitor) \u9078\u64c7\u6027\u6291\u5236\u5291<strong><u>\u00a0<\/u><\/strong><\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS#\u00a01243583-85-8<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865f\u00a0B3276<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">HAT inhibitor<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34002\">4&#8242;-bromo-Resveratrol<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\"><a style=\"color: #000080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34002\">CAS# 1224713-90-9\u00a0<\/a><\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865f C3552<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">Sirt1 \u548c Sirt3 \u6291\u5236\u5291<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34010\">MS023<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS# 1831110-54-3<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865f B6183<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">type I PRMTs inhibitor\u6291\u5236\u5291<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=34348\">CHZ868<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">N\/O<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865fB5980<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">Type II JAK2 inhibitor<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35251\">Chidamide<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS#743420-02-2<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865fB5916<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">Novel HDAC inhibitor<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35254\">RGFP966<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS#1357389-11-7\/1396841-57-8<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865fA8803<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">Specific HDAC3 inhibitor<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35260\">EPZ-6438<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS#1403254-99-8<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865fA8221<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">EZH2 inhibitor, potent and selective<\/span><\/td>\n<\/tr>\n<tr>\n<td width=\"139\"><span style=\"color: #008080;\"><a style=\"color: #008080;\" href=\"http:\/\/biopioneer.com.tw\/?p=35291\">Bromodomain Inhibitor, (+)-JQ1<\/a><\/span><\/td>\n<td width=\"139\"><span style=\"color: #000080;\">CAS# 1268524-70-4<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">\u8ca8\u865fA1910<\/span><\/td>\n<td width=\"138\"><span style=\"color: #000080;\">BET bromodomain inhibitor<\/span><\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>APExBIO\u53f0\u7063\u4ee3\u7406\u5546 APExBIO\u63d0\u4f9b\u512a\u8cea\u7684\u80dc\u80bd\u548c\u751f\u7269\u5206\u6790\u8a66\u5291\uff0c\u5ee3\u6cdb\u7522\u54c1\u7dda\u5982Protease\u3001Chrom [&hellip;]<\/p>\n","protected":false},"author":3,"featured_media":34308,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[5368,3],"tags":[5022],"_links":{"self":[{"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35318"}],"collection":[{"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=35318"}],"version-history":[{"count":4,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35318\/revisions"}],"predecessor-version":[{"id":51817,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35318\/revisions\/51817"}],"wp:featuredmedia":[{"embeddable":true,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/34308"}],"wp:attachment":[{"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=35318"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=35318"},{"taxonomy":"post_tag","embeddable":true,"href":"http:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=35318"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}