1. AR-42为本公司优势产品，可申请免费样品
2. 极速发货，高效助力生产
3. 品质保证,稳定供应
4. 支持验收后付款
| 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) |
| AR-42 | |
|---|---|
| 参数 | 数值 |
| 密度 | 1.223 |
邻氨基噻吩(2盐酸)(90069-81-1 ) | 2-氟-3-硝基吡啶(1480-87-1 ) | 环氧琥珀酸聚合物(51274-37-4 ) | 对氟苯甲酰氯(403-43-0 ) | 丹参总酮 | 1-硼酸频哪醇酯-4-乙酸乙酯-1-环已烯(1166829-70-4 ) | 1,2-丙二醇单十二酸酯(27194-74-7 ) | 他卡西妥(57333-96-7 ) | 2-脱氧-2,2-二氟戊呋喃糖-1-酮 3,5-二安息香酸盐(122111-01-7 ) | 1,8-二氨基-3,6-二氧杂辛烷(929-59-9 ) |
