| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408722-1ml |
1ml |
现货  |
|
| 英文别名 | HDAC-42 | (S)-N-hydroxy-4-(3-methyl-2-phenylbutanamido)benzamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | AR-42 |
| 生化机理 | AR-42 （HDAC-42）是一种 HDAC 抑制剂，IC50 为 30 nM。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
AR-42 (OSU-HDAC42)，hydroxamate-tethered phenylbutyrate的衍生物，是一种新型有效的组蛋白去乙酰化酶（HDAC）抑制剂，有效抑制HDAC的活性，IC50值为16 nM，诱导组蛋白H3乙酰化，α-微管蛋白乙酰化和p21的上调，这些被视为HDAC抑制的标志性指标。据报道，AR-42调节几个细胞凋亡抑制剂以及细胞存活调节剂，包括Akt、Bcl-xL、Bax、Ku70和Surviving，通过对PI3K/Akt信号通路的至少部分抑制，对多种肿瘤类型具有有效的抗肿瘤活性，如人前列腺癌和肝癌。 AR-42 (HDAC-42) 是一种HDAC抑制剂，IC50为30 nM。 Information AR-42 AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1. 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. In vivo 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. cell lines：Differentiated HL60 (dHL60) cells Concentrations：Dissolved in DMSO, final concentrations ~2.5 μM Incubation Time：96 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC(C)[C@@H](C1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)C(=O)NO |
| 分子量 | 312.36 |
| Reaxy-Rn | 15600115 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15600115&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (64.48 mM); Water: 100 mg/mL (64.48 mM); Ethanol: 50 mg/mL (32.24 mM); |
|---|
| 象形图 | GHS08, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H302: 吞食有害 H332: 吸入有害 H360: 可能损害生育力或未出生的孩子 H312+H332: 皮肤接触或吸入有害。 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。 P317: 寻求紧急医疗救助。 |
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