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AR42

AR42

产品编号 T6392   CAS 935881-37-1
别名: OSU-HDAC42, AR-42, (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺, AR 42, HDAC-42

AR42 (OSU-HDAC42) 是一种 HDAC 抑制剂(IC50: 30 nM)。

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AR42 Chemical Structure
AR42, CAS 935881-37-1
规格 价格/CNY 货期 数量
1 mg ¥ 326 现货
2 mg ¥ 468 现货
5 mg ¥ 787 现货
10 mg ¥ 1,320 现货
25 mg ¥ 2,430 现货
50 mg ¥ 3,690 现货
100 mg ¥ 5,180 现货
200 mg ¥ 7,120 现货
1 mL * 10 mM (in DMSO) ¥ 865 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: AR42 (T6392)
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纯度: 99.46%
纯度: 98.96%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 AR42 (OSU-HDAC42) is an HDAC inhibitor (IC50: 30 nM).
靶点活性 HDAC:30 nM
体外活性 AR-42 induces p21WAF/CIP1 overexpression and histone hyperacetylation and inhibits the growth of DU-145 cells (IC50 of 0.11 μM) [1]. AR-42 is effective in suppressing the proliferation of PC-3 and U87 mg cells, in part, because of its ability to down-regulate Akt signaling [2]. AR-42 inhibits the growth of PC-3 (IC50: 0.48 μM) and LNCaP (IC50: 0.3 μM) cells. Compared to SAHA, AR-42 has markedly superior apoptogenic potency and causes obviously greater decreases in Bcl-xL, phospho-Akt, and survivin in PC-3 cells [3]. in malignant mast cell lines, AR-42 induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5 [6]. AR-42 effectively inhibits the growth of Raji, JeKo-1, and 697 cells (IC50<0.61 μM). AR-42 also sensitizes CLL cells to TNF-Related Apoptosis-Inducing Ligand (TRAIL), potentially through reduction of c-FLIP [7]. AR-42 also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in HCC cells.
体内活性 The growth of PC-3 tumor xenografts is suppressed by 52% and 67% after treatment with AR-42 (25/50 mg/kg), respectively, whereas SAHA (50 mg/kg) suppresses growth by 31%. In contrast to mice treated with SAHA, intratumoral levels of Bcl-xL and pAkt are markedly reduced in AR-42 treated mice. [3] In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, 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 (86%) and relative (85%) urogenital tract weights. [5] AR-42 markedly reduces leukocyte counts and prolongs survival in three separate mouse models of B-cell malignancy without toxicity.
激酶实验 In vitro HDAC assay:HDAC activity is analyzed by using an HDAC assay kit. This assay is based on the ability of DU-145 nuclear extract, which is rich in HDAC activity, to mediate the deacetylation of the biotinylated [3H]-acetyl histone H4 peptide that is bound to streptavidin agarose beads. The release of [3H]-acetate into the supernatant is measured to calculate the HDAC activity. Sodium butyrate (0.25-1 mM) is used as a positive control.
细胞实验 Concentrations: Dissolved in DMSO,final concentrations ~2.5 μM. Method: DU-145 Cells are exposed to various concentrations of AR-42 for 96 hours.The medium is removed and replaced by 150 μL of 0.5 mg/mL of MTT in RPMI 1640 medium,and the cells are incubated in the CO2 incubator at 37 °C for 2 hours.Supernatants are removed from the wells,and the reduced MTT dye is solubilized with 200 μL/well of DMSO.Absorbance is determined on a plate reader at 570 nm.
动物实验 Animal Models: Intact male NCr athymic nude mice inoculated s.c.with PC-3 cells. Formulation: Formulated in methylcellulose/Tween 80. Dosages: ~50 mg/kg/day. Administration: p.o.
别名 OSU-HDAC42, AR-42, (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺, AR 42, HDAC-42
分子量 312.36
分子式 C18H20N2O3
CAS No. 935881-37-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 59 mg/mL (188.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 59 mg/mL (188.9 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.2014 mL 16.0072 mL 32.0143 mL 80.0359 mL
5 mM 0.6403 mL 3.2014 mL 6.4029 mL 16.0072 mL
10 mM 0.3201 mL 1.6007 mL 3.2014 mL 8.0036 mL
20 mM 0.1601 mL 0.8004 mL 1.6007 mL 4.0018 mL
50 mM 0.064 mL 0.3201 mL 0.6403 mL 1.6007 mL
100 mM 0.032 mL 0.1601 mL 0.3201 mL 0.8004 mL

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TargetMol Library Books参考文献

1. Lu Q, et al. J Med Chem, 2005, 48(17), 5530-5535. 2. Chen CS, et al. J Biol Chem, 2005, 280(46), 38879-38887. 3. Kulp SK, et al. Clin Cancer Res, 2006, 12(17), 5199-5206. 4. Chen CS, et al. Cancer Res, 2007, 67(11), 5318-5327. 5. Sargeant AM, et al. Cancer Res, 2008, 68(10), 31999-42009. 6. Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7(16):22285-94. 7. Su L, Wang S, Yuan T, et al. Anti-oral Squamous Cell Carcinoma Effects of a Potent TAZ Inhibitor AR-42[J]. Journal of Cancer. 2020, 11(2): 364-373. 8. Zhu Y, Yuan T, Zhang Y, et al. AR-42:A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321.

TargetMol Library Books文献引用

1. Zhu Y, Yuan T, Zhang Y, et al. AR-42: A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321 2. Zhu Y, Yuan T, Zhang Y, et al. AR-42: A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321 3. Su L, Wang S, Yuan T, et al. Anti-oral Squamous Cell Carcinoma Effects of a Potent TAZ Inhibitor AR-42. Journal of Cancer. 2020, 11(2): 364-373.
HDAC8-IN-4 Panobinostat HDAC-IN-60 Quisinostat dihydrochloride TMP269 Divalproex Sodium CRA-026440 Exifone

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗癌药物库 抗癌临床化合物库 抑制剂库 抗癌活性化合物库 抗癌化合物库 抗乳腺癌化合物库 经典已知活性库 NF-κB 通路分子库 已知活性化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AR42 935881-37-1 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC OSU-HDAC42 HDAC 42 HDAC42 AR-42 (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺 AR 42 HDAC-42 Inhibitor inhibitor inhibit

 

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