用途
AR-42 |
参数 | 数值 |
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 p21WAF/CIP1 overexpression, inhibits the growth of DU-145 cells with IC50 of 0.11 μM. HDAC42 is potent in suppressing the proliferation of U87MG PC-3 cells, in part, because of its ability to down-regulate Akt signaling. AR-42 inhibits the growth of PC-3 LNCaP cells with IC50 of 0.48 μM 0.3 μM, respectively. Compared to SAHA, AR-42 exhibits distinctly superiapoptogenic potency, causes markedly greater decreases in phospho-Akt, Bcl-xL, survivin in PC-3 cells. AR-42 treatment induces growth inhibition, cell- cycle arrest, apoptosis, 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 heat shock protein 90 (HSP90), up-regulation of HSP70. AR-42 treatment down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), total STAT3/5. AR-42 potently inhibits the growth of JeKo-1, Raji, 697 cells with IC50 of <0.61 μM. AR-42 also sensitizes CLL cells to TNF-Related Apoptosis Inducing Lig(TRAIL), potentially through reduction of c-FLIP. AR-42 treatment also induces autophagy through downregulation of Akt/mTsignaling inducing ER stress in hepatocellular carcinoma (HCC) cells. | 体内研究 | The growth of PC-3 tumxenografts is suppressed by 52% 67% after treatment with AR-42 at 25 mg/kg 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 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) completely prevents its progression to poorly differentiated carcinoma, but also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute relative urogenital tract weights by 86% 85%, respectively. AR-42 significantly reduces leukocyte counts, prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity. | 特征 | More potent than SAHA. | 别名 | (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺 | 英文别名 | AR-42;(S)-HDAC-42,AR-42;(S)-(+)-N-Hydroxy-4-(3-methyl-2-phenyl-butyrylamino)benzamide;(S)-HDAC42;AR-42(HDAC-42);HDAC-42;OSU-HDAC42;AR-42(OSU-HDAC42) | |
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供应 935881-37-1 | 供应 AR-42 | 现货 935881-37-1 | 现货 AR-42 | 高纯 935881-37-1 | 高纯 AR-42 | 定制 935881-37-1 | 定制 AR-42 | 935881-37-1 供应商 | AR-42 供应商 | 935881-37-1 生产厂家 | AR-42 生产厂家 | 935881-37-1 价格 | AR-42 价格 | 935881-37-1 现货 | AR-42 现货 | 935881-37-1 作用 | AR-42 作用 | 935881-37-1 原料 | AR-42 原料 | 935881-37-1 定制 | AR-42 定制 | 935881-37-1 试剂 | AR-42 试剂 |
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