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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
- 库存:
99
- 供应商:
爱必信(上海)生物科技有限公司
- CAS号:
935881-37-1
- 规格:
10mg/5mg
| 规格: | 10mg | 产品价格: | ¥2115.0 |
|---|---|---|---|
| 规格: | 5mg | 产品价格: | ¥1184.0 |
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抑制剂描述: 产品名称:AR-42 产品别名:见爱必信官网 英文别名:AR-42 靶点:HDAC CAS:935881-37-1 纯度:99% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: AR-42 is a novel HDAC inhibitor with an IC50 of 0.61 μM for acute lymphoblastic leukemia (697) cell lines. 溶解性:DMSO:40 mg/mL 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 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.
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文献和实验5.99 5.82 5.69 5.60 5.52 5.46 5.37 5.27 5.17 5.06 4.96 4.85 6 7 6.54 5.89 5.52 5.28 5.12 4.99 4.90 4.82 4.76 4.67 4.57 4.47 4.36 4.25 4.14 7 8 6.06 5.42 5.05 4.82 4.65 4.53 4.43 4.36 4.29 4.20 4.10 4.00 3.89 3.78 3.67 8 9 5.71 5.08 4.72 4.48
30分钟,以除去细胞有形成份。活活性荧光法测定步骤:AR活性测定的反应体系包括以下成分(最终浓度):67mmol/l的钠—钾磷酸缓冲液(pH 7.0),0.2mol/l 硫酸铵,0.1mmol/lNADPH,10mmol/l DL-甘油醛和红细胞溶血液10ul,总体积1.0ml.空白管以双蒸水代替DL—甘油醛。在37℃水浴反应5分钟后加0.3mol/l的NAOH2ml终止反应。充分混匀后60℃加热15分钟,破坏NADPH然后加11.8mol/l NAOH[内含0.1%H2O2) 3.0ml充分混匀
一、SP 法 1)脱蜡、水化;2)PBS 洗 2~3 次各 5 分钟;3)3% H2O2(80% 甲醇)滴加在 TMA 上,室温静置 10 分钟;4)PBS 洗 2~3 次各 5 分钟;5)抗原修复;6)PBS 洗 2~3 次各5分钟;7)滴加正常山羊血清封闭液,室温 20 分钟。甩去多余液体。8)滴加Ⅰ抗 50μl,室温静置 1 小时或者4℃过夜或者37℃1小时。9)4℃ 过夜后需在37℃复温45分钟。10)PBS 洗 3 次各 5 分钟;11)滴加 Ⅱ 抗 40~50 μl,室温
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