{"id":43206,"date":"2023-06-18T10:01:15","date_gmt":"2023-06-18T02:01:15","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=43206"},"modified":"2023-06-27T11:27:38","modified_gmt":"2023-06-27T03:27:38","slug":"jnj-26481585-potent-hdac-inhibitor-cas875320-29-9-apexbio%e8%b2%a8%e8%99%9fa4090","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=43206","title":{"rendered":"HDAC\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176\u6291\u5236\u5291 | JNJ-26481585 Potent HDAC inhibitor CAS#875320-29-9 APExBIO\u8ca8\u865fA4090"},"content":{"rendered":"

JNJ-26481585 Potent HDAC inhibitor CAS#875320-29-9 APExBIO\u8ca8\u865fA4090<\/span><\/a><\/span><\/strong><\/p>\n

Potent HDAC inhibitor- HDAC1\u3001HDAC2\u00a0 and HDAC3<\/p>\n

\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176 (Histone deacetylase, HDAC) \u6291\u5236\u5291 \u65b0\u578b\u6297\u764c\u5291<\/span><\/span><\/strong><\/span><\/p>\n

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\u7d44\u86cb\u767d\u812b\u4e59\u91af\u9176 (Histone deacetylase, HDAC) \u6291\u88fd\u5291(inhibitors)\u662f\u4e00\u985e\u76f8\u5c0d\u8f03\u65b0\u7684\u6297\u764c\u5291\uff0c\u5728\u8868\u89c0\u907a\u50b3(epigenetic )\u6216\u975e\u8868\u89c0\u907a\u50b3\u8abf\u63a7(non-epigenetic regulation)\u3001\u8a98\u5c0e\u764c\u7d30\u80de\u6b7b\u4ea1(death)\u3001\u7d30\u80de\u51cb\u4ea1(apoptosis)\u548c\u7d30\u80de\u9031\u671f\u505c\u6eef(cell cycle arrest)\u65b9\u9762\u767c\u63ee\u91cd\u8981\u4f5c\u7528\u3002\u6700\u8fd1\uff0c\u5b83\u5011\u7684\u4f7f\u7528\u5df2\u5728\u764c\u75c7\u60a3\u8005\u4e2d\u5f97\u5230\u81e8\u5e8a\u9a57\u8b49\uff0c\u5c0e\u81f4\u5169\u7a2e HDAC \u6291\u5236\u5291\u4f0f\u7acb\u8afe\u4ed6(vorinostat<\/a><\/span>)\u548c depsipetide \u7372\u5f97 FDA \u7684\u6279\u51c6\u3002\u6b64\u5916\uff0c\u5e7e\u7a2e\u7528\u4f5c\u6297\u764c\u85e5\u7269\u55ae\u7368\u6216\u8207\u5176\u4ed6\u6297\u764c\u7642\u6cd5(anti-cancer therapeutics)\u806f\u5408\u4f7f\u7528\uff0c HDAC \u6291\u88fd\u5291\u7684\u81e8\u5e8a\u8a66\u9a57\u6b63\u5728\u9032\u884c\u4e2d\u3002\u7136\u800c\uff0c\u764c\u75c7\u60a3\u8005\u5c0d HDAC \u6291\u5236\u5291\u53cd\u61c9\u7684\u5206\u5b50\u6a5f\u5236\u5c1a\u4e0d\u5b8c\u5168\u6e05\u695a\u3002<\/p>\n

<\u8cc7\u6599\u4f86\u6e90 https:\/\/www.ncbi.nlm.nih.gov\/pmc\/articles\/PMC3056563\/><\/span><\/p>\n

JNJ-26481585\u7522\u54c1\u4ecb\u7d39<\/span><\/strong><\/span><\/p>\n

JNJ-26481585 \u662f\u4e00\u7a2e\u65b0\u578b\u7d44\u86cb\u767d\u53bb\u4e59\u91af\u5316\u9176 (novel histone deacetylase, HDAC) \u6291\u5236\u5291\uff0c\u5c0d I \u985e HDAC\uff08\u5305\u62ec HDAC1\u3001HDAC2 \u548c HDAC3\uff09\u5177\u6709\u5f88\u5f37\u7684\u6548\u529b\uff0c\u6291\u5236\u5e38\u6578 IC50 \u503c\u5206\u5225\u70ba 0.11\u30010.33 \u548c 4.8 nmol\/L\uff0c\u5c0e\u81f4\u5f37\u70c8\u7684\u6297\u589e\u6b96\u6d3b\u6027( anti-proliferative activities ) \uff08IC50 \u7bc4\u570d\u5f9e 3.1 \u5230 246 nmol\/L\uff09\u91dd\u5c0d\u5ee3\u6cdb\u7684\u764c\u7d30\u80de\u7cfb\uff0c\u5305\u62ec\u80ba\u764c( lung)\u3001\u4e73\u817a\u764c(breast)\u3001\u7d50\u8178\u764c( colon)\u3001\u524d\u5217\u817a\u764c(prostate)\u3001\u8166\u764c(brain )\u548c\u53e3\u8154\u764c\u7d30\u80de\u682a ( overian cancer cell lines)\u3002\u6700\u8fd1\u7684\u7814\u7a76\u7d50\u679c\u8868\u660e\uff0cJNJ-26481585 \u5728\u9ad4\u5167\u5f37\u70c8\u8a98\u5c0e HDAC1 \u6291\u5236\u7684 p21waf1\u3001cip1 \u555f\u52d5\u5b50\u3001\u816b\u7624\u7d44\u7e54\u4e2d\u7684\u7d44\u86cb\u767d H3 \u4e59\u91af\u5316\u548c\u9ad4\u5916\u4eba\u7d50\u8178\u764c\u7d30\u80de\u682a(human colon cancer cell lines)\uff08APC \u91ce\u751f\u578b\u548c\u7a81\u8b8a\u9ad4\uff09\u7684\u7d30\u80de\u51cb\u4ea1\u3002<\/p>\n

\u91cd\u7d44 HDAC \u6d3b\u6027\u6e2c\u5b9a\u7531 Reaction Biology Corporation \u5b8c\u6210\u3002\u5728\u6240\u6709\u60c5\u6cc1\u4e0b\uff0c\u5168\u9577 HDAC \u86cb\u767d\u5747\u4f7f\u7528\u687f\u72c0\u75c5\u6bd2\u611f\u67d3\u7684 Sf9 \u7d30\u80de\u8868\u9054\u3002\u6b64\u5916\uff0cHDAC3 \u8207\u4eba\u985e NCOR2 \u5171\u8868\u9054\u70ba\u8907\u5408\u7269\u3002\u70ba\u4e86\u8a55\u4f30\u542b HDAC1 \u7684\u7d30\u80de\u8907\u5408\u7269\u7684\u6d3b\u6027\uff0c\u5c07\u514d\u75ab\u6c89\u6fb1\u7684 HDAC1 \u8907\u5408\u7269\u8207\u7d44\u86cb\u767d H4 \u80bd [\u751f\u7269\u7d20-(6-\u6c28\u57fa\u5df1\u9178)Gly-Ala-(\u4e59\u9170[3H])Lys-Arg-His-\u7684 [3H] \u4e59\u9170\u6a19\u8a18\u7247\u6bb5\u4e00\u8d77\u5b75\u80b2Arg-Lys-Val-NH2]\u3002\u5982\u86cb\u767d\u8cea\u5370\u8de1\u5206\u6790\u6240\u793a\uff0c\u514d\u75ab\u6c89\u6fb1\u7b49\u91cf\u7684 HDAC1\u3002 HDAC1 \u6d3b\u6027\u7d50\u679c\u8868\u793a\u70ba\u5c0d\u55ae\u500b\u88c2\u89e3\u7269\u9032\u884c\u7684\u4e09\u500b\u7368\u7acb\u5be6\u9a57\u7684\u5e73\u5747\u503c\u00b1\u6a19\u6e96\u5dee\u3002<\/p>\n

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<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Storage<\/td>\nStore at -20\u00b0C<\/td>\n<\/tr>\n
M.Wt<\/td>\n394.47<\/td>\n<\/tr>\n
Cas No.<\/td>\n875320-29-9<\/td>\n<\/tr>\n
Formula<\/td>\nC21<\/sub>H26<\/sub>N6<\/sub>O2<\/sub><\/td>\n<\/tr>\n
Synonyms<\/td>\nJNJ26481585<\/td>\n<\/tr>\n
Solubility<\/td>\ninsoluble in H2O; insoluble in EtOH; \u226519.2 mg\/mL in DMSO<\/td>\n<\/tr>\n
Chemical Name<\/td>\nN-hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide<\/td>\n<\/tr>\n
SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
Canonical SMILES<\/td>\nCN(C=C1CNCC2CCN(C3=NC=C(C(NO)=O)C=N3)CC2)C4=C1C=CC=C4<\/td>\n<\/tr>\n
Shipping Condition<\/td>\nSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.<\/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
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Product Citation<\/span><\/strong><\/span><\/h2>\n<\/div>\n
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