{"id":35260,"date":"2022-10-24T14:24:57","date_gmt":"2022-10-24T06:24:57","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=35260"},"modified":"2025-11-15T15:59:58","modified_gmt":"2025-11-15T07:59:58","slug":"epz-6438-cas1403254-99-8-apexbio-%e8%b2%a8%e8%99%9fa8221","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=35260","title":{"rendered":"EPZ-6438 | CAS#1403254-99-8 APExBIO \u8ca8\u865fA8221"},"content":{"rendered":"

\u8868\u89c0\u907a\u50b3\u5b78(Epigenetics)\u7cfb\u5217\u5546\u54c1->>EPZ-6438<\/span><\/span><\/span><\/span><\/strong><\/p>\n

APExBIO Technology LLC \u662f\u4e00\u5bb6\u9818\u5148\u7684\u5c0f\u5206\u5b50\u6291\u5236\u5291 (Small Molecule Inhibitors)\/\u6d3b\u5316\u5291(Activators)\u3001\u5316\u5408\u7269\u5eab( Compound Libraries)\u3001\u80dc\u80bd(Peptides)\u3001\u6aa2\u6e2c\u8a66\u5291\u76d2(Assay Kits)\u3001\u87a2\u5149\u6a19\u8a18(Fluorescent Label)\u3001\u9176(Enzymes)\u3001\u4fee\u98fe\u6838\u82f7\u9178(Modified Nucleotides)\u3001mRNA \u5408\u6210\u4ee5\u53ca\u5404\u7a2e\u5206\u5b50\u751f\u7269\u5b78\u5de5\u5177\u7684\u4f9b\u61c9\u5546\u3002APExBIO\u63d0\u4f9b\u5ee3\u6cdb\u7684\u7522\u54c1\u7dda\uff0c\u6db5\u84cb 20 \u591a\u500b\u4e0d\u540c\u7684\u7814\u7a76\u9818\u57df\uff0c\u4f8b\u5982\u764c\u75c7(cancer)\u3001\u514d\u75ab\u5b78(immunology)\u3001\u795e\u7d93\u79d1\u5b78(neurosciences)\u3001\u7d30\u80de\u51cb\u4ea1(apoptosis)\u548c\u8868\u89c0\u907a\u50b3\u5b78(epigenetics)\u7b49\u3002\u516c\u53f8\u7e3d\u90e8\u4f4d\u65bc\u7f8e\u570b\u5fb7\u5dde\u4f11\u58eb\u9813USA (Houston, Texas)\uff0c\u81f4\u529b\u65bc\u670d\u52d9\u5168\u7403\u5ba2\u6236\u3002\u9ad8\u5ea6\u91cd\u8996\u7522\u54c1\u54c1\u8cea\u3002\u6240\u6709\u7522\u54c1\u5747\u9075\u5faa\u56b4\u683c\u7684\u751f\u7522\u6307\u5357\uff0c\u4e26\u9644\u6709\u5206\u6790\u8b49\u66f8\u3001HPLC\u3001\u8cea\u8b5c(Mass Spectrum)\u548cHMNR\u4ee5\u53ca\u9ad4\u5916\u9a57\u8b49(in vitro validation)\u3002 APExBIO\u7522\u54c1\u5df2\u88ab\u300aNature\u300b\u3001\u300aCell\u300b\u548c\u300aScience\u300b\u7b49\u773e\u591a\u9802\u7d1a\u540c\u884c\u8a55\u5be9\u671f\u520a\u5f15\u7528\u3002>>\u66f4\u591aAPExBio\u5546\u54c1<\/span><\/strong><\/em><\/span><\/a><\/p>\n

<\/p>\n

Chromatin\/Epigenetics\u7cfb\u5217\u7522\u54c1+<\/span><\/strong><\/span><\/p>\n

\"\"<\/p>\n

\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

\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

\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\u3002<\/p>\n

EPZ-6438 | CAS#1403254-99-8 APExBIO\u00a0 \u8ca8\u865fA8221<\/a><\/span><\/p>\n

EZH2 inhibitor, potent and selective<\/p>\n

\"\"<\/p>\n

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>\n

Product Citation+6<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Physical Appearance<\/td>\nA solid<\/td>\n<\/tr>\n
Storage<\/td>\nDesiccate at -20\u00b0C<\/td>\n<\/tr>\n
M.Wt<\/td>\n572.74<\/td>\n<\/tr>\n
Cas No.<\/td>\n1403254-99-8<\/td>\n<\/tr>\n
Formula<\/td>\nC34<\/sub>H44<\/sub>N4<\/sub>O4<\/sub><\/td>\n<\/tr>\n
Synonyms<\/td>\nE-7438<\/td>\n<\/tr>\n
Solubility<\/td>\n\u226528.64 mg\/mL in DMSO; insoluble in EtOH; insoluble in H2O<\/td>\n<\/tr>\n
Chemical Name<\/td>\nN-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide<\/td>\n<\/tr>\n
SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
Canonical SMILES<\/td>\nCCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5<\/td>\n<\/tr>\n
Shipping Condition<\/td>\nShip with blue ice, or upon other requests.<\/td>\n<\/tr>\n
General tips<\/td>\nFor obtaining a higher solubility, please warm the tube at 37\u00b0C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

 <\/p>\n

    \n
  1. Fumiya Moribe, Momoko Nishikori, et al. “Epigenetic suppression of SLFN11 in germinal center B-cells during B-cell development.” PLoS One. 2021 Jan 29;16(1):e0237554.PMID:33513156<\/a><\/li>\n
  2. Otsuka Y, Nishikori M, et al. “EZH2 inhibitors restore epigenetically silenced CD58 expression in B-cell lymphomas.” Mol Immunol. 2020;119:35\u201345.PMID:31962268<\/a><\/li>\n
  3. Anastassiia Vertii, Jianhong Ou, et al. “Two Contrasting Classes of Nucleolus-Associated Domains in Mouse Fibroblast Heterochromatin.” bioRxiv. 2018 December 03.<\/li>\n
  4. Jiang S, Zhou H, et al. “The Epstein-Barr Virus Regulome in Lymphoblastoid Cells.” Cell Host Microbe. 2017 Oct 11;22(4):561-573.e4.PMID:29024646<\/a><\/li>\n
  5. Arifuzzaman S, Das A, et al. “Selective inhibition of EZH2 by a small molecule inhibitor regulates microglial gene expression essential for inflammation.” Biochem Pharmacol. 2017 Apr 19. pii: S0006-2952(17)30233-2.PMID:28431938<\/a><\/li>\n
  6. Wang H, Tian L, et al. “Bone-in-culture array as a platform to model early-stage bone metastases and discover anti-metastasis therapies.” Nat Commun. 2017 Apr 21;8:15045.PMID:28429794<\/a><\/li>\n<\/ol>\n

    <\/p>\n

    APExBIO\u53f0\u7063\u4ee3\u7406\u5546:\u00a0 <\/span><\/span><\/strong><\/span><\/a>https:\/\/www.apexbt.com\/<\/span><\/span><\/a><\/span><\/p>\n

    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\u3002
    \n\"\u578b\u9304\u4e0b\u8f09\"<\/a><\/p>\n\n\n\n\n\n\n\n\n\n\n\n
    \u54c1\u9805<\/span><\/td>\nCAS#<\/span><\/td>\n#\u8ca8\u865f<\/span><\/td>\n\u61c9\u7528<\/span><\/td>\n<\/tr>\n
    MG 149 \u00a0(Tip60 HAT inhibitor) \u9078\u64c7\u6027\u6291\u5236\u5291\u00a0<\/u><\/strong><\/a><\/span><\/td>\nCAS#\u00a01243583-85-8<\/span><\/td>\n\u8ca8\u865f\u00a0B3276<\/span><\/td>\nHAT inhibitor<\/span><\/td>\n<\/tr>\n
    4′-bromo-Resveratrol<\/a><\/span><\/td>\nCAS# 1224713-90-9\u00a0<\/a><\/span><\/td>\n\u8ca8\u865f C3552<\/span><\/td>\nSirt1 \u548c Sirt3 \u6291\u5236\u5291<\/span><\/td>\n<\/tr>\n
    MS023<\/a><\/span><\/td>\nCAS# 1831110-54-3<\/span><\/td>\n\u8ca8\u865f B6183<\/span><\/td>\ntype I PRMTs inhibitor\u6291\u5236\u5291<\/span><\/td>\n<\/tr>\n
    CHZ868<\/a><\/span><\/td>\nN\/O<\/span><\/td>\n\u8ca8\u865fB5980<\/span><\/td>\nType II JAK2 inhibitor<\/span><\/td>\n<\/tr>\n
    Chidamide<\/a><\/span><\/td>\nCAS#743420-02-2<\/span><\/td>\n\u8ca8\u865fB5916<\/span><\/td>\nNovel HDAC inhibitor<\/span><\/td>\n<\/tr>\n
    RGFP966<\/a><\/span><\/td>\nCAS#1357389-11-7\/1396841-57-8<\/span><\/td>\n\u8ca8\u865fA8803<\/span><\/td>\nSpecific HDAC3 inhibitor<\/span><\/td>\n<\/tr>\n
    EPZ-6438<\/a><\/span><\/td>\nCAS#1403254-99-8<\/span><\/td>\n\u8ca8\u865fA8221<\/span><\/td>\nEZH2 inhibitor, potent and selective<\/span><\/td>\n<\/tr>\n
    Bromodomain Inhibitor, (+)-JQ1<\/a><\/span><\/td>\nCAS# 1268524-70-4<\/span><\/td>\n\u8ca8\u865fA1910<\/span><\/td>\nBET bromodomain inhibitor<\/span><\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

     <\/p>\n","protected":false},"excerpt":{"rendered":"

    \u8868\u89c0\u907a\u50b3\u5b78(Epigenetics)\u7cfb\u5217\u5546\u54c1->>EPZ-6438 APExBIO Technol […]<\/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":[5019],"_links":{"self":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35260"}],"collection":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=35260"}],"version-history":[{"count":7,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35260\/revisions"}],"predecessor-version":[{"id":53776,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35260\/revisions\/53776"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/34308"}],"wp:attachment":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=35260"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=35260"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=35260"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}