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AR-42

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AR-42 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 英文名称:AR-42
CAS:935881-37-1
公司名称: 百灵威科技有限公司  
联系电话: 400-666-7788 +86-10-82848833
产品介绍: 英文名称:AR-42
CAS:935881-37-1
包装信息:100Mg,10Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称: 上海佰世凯化学科技有限公司  
联系电话: +86(0)21-20908456
产品介绍: 英文名称:AR 42
CAS:935881-37-1
备注:C14654
公司名称: BOC Sciences  
联系电话:
产品介绍: 英文名称:AR-42
CAS:935881-37-1
公司名称: T&W GROUP  
联系电话: +86-21-61551611, 61551462, 61551420, 61551610
产品介绍: 英文名称:(S)-HDAC-42
CAS:935881-37-1
纯度:98% 包装信息:100g;500g;1kg;5kg;10kg
最新发布供应信息
AR-42_上海楼岚生物科技有限公司
2019/3/13 16:56:07
935881-37-1_上海昶衍化工科技有限公司
2012/3/21 16:40:14
AR-42
生物活性 体外研究 体内研究 特征
中文名称:AR-42
中文同义词:(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺
英文名称:AR-42
英文同义词:AR-42;(S)-HDAC-42,AR-42;(S)-(+)-N-Hydroxy-4-(3-methyl-2-phenyl-butyrylamino)benzamide;(S)-HDAC 42;AR-42 (HDAC-42);HDAC-42;NSC-D736012;OSU-HDAC42
CAS号:935881-37-1
分子式:C18H20N2O3
分子量:312.363
EINECS号:802-219-4
相关类别:小分子抑制剂,天然产物;表观遗传学;Inhibitor;Inhibitors
Mol文件:935881-37-1.mol
AR-42
AR-42 性质
密度 1.223
AR-42 用途与合成方法
生物活性AR-42是一种HDAC抑制剂,IC50为30 nM。Phase 1。
体外研究AR-42 treatment induces histone hyperacetylation and p21WAF/CIP1 overexpression, and inhibits the growth of DU-145 cells with IC50 of 0.11 μM. HDAC42 is potent in suppressing the proliferation of U87MG and PC-3 cells, in part, because of its ability to down-regulate Akt signaling. AR-42 inhibits the growth of PC-3 and LNCaP cells with IC50 of 0.48 μM and 0.3 μM, respectively. Compared to SAHA, AR-42 exhibits distinctly superior apoptogenic potency, and causes markedly greater decreases in phospho-Akt, Bcl-xL, and survivin in PC-3 cells. AR-42 treatment induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7 in malignant mast cell lines. AR-42 treatment induces down-regulation of Kit via inhibition of Kit transcription, disassociation between Kit and heat shock protein 90 (HSP90), and up-regulation of HSP70. AR-42 treatment down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5. AR-42 potently inhibits the growth of JeKo-1, Raji, and 697 cells with IC50 of <0.61 μM. AR-42 also sensitizes CLL cells to TNF-Related Apoptosis Inducing Ligand (TRAIL), potentially through reduction of c-FLIP. AR-42 treatment also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in hepatocellular carcinoma (HCC) cells.
体内研究The growth of PC-3 tumor xenografts is suppressed by 52% and 67% after treatment with AR-42 at 25 mg/kg and 50 mg/kg, respectively, whereas SAHA at 50 mg/kg suppresses growth by 31%. In contrast to mice treated with SAHA, intratumoral levels of phospho-Akt and Bcl-xL are markedly reduced in AR-42 treated mice. In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, administration of AR-42 not only decreases the severity of prostatic intraepithelial neoplasia (PIN) and completely prevents its progression to poorly differentiated carcinoma, but also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute and relative urogenital tract weights by 86% and 85%, respectively. AR-42 significantly reduces leukocyte counts, and prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity.
特征More potent than SAHA.
安全信息
"AR-42" 相关产品信息
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