AR42

产品编号: T6392 别名:

OSU-HDAC42,HDAC-42,AR-42,(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺,AR 42

AR42 是一种 HDAC 抑制剂 (IC50: 30 nM)。

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CAS：935881-37-1

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

AR-42 is an HDAC inhibitor (IC50: 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.

Cas No.

935881-37-1

分子式

C18H20N2O3

分子量

312.36

别名

OSU-HDAC42;HDAC-42;AR-42;(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺;AR 42;AR42

参考文献

[1]Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7(16):22285-94.[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]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.[6]Lu Q, et al. J Med Chem, 2005, 48(17), 5530-5535.[7]Sargeant AM, et al. Cancer Res, 2008, 68(10), 31999-42009.[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.

引用文献

[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.

储存和溶解度

Ethanol:59 mg/mL (188.9 mM)
H2O:<1 mg/mL
DMSO:59 mg/mL (188.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 AR42 935881-37-1

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

第一步：请输入动物实验的基本信息

剂量 mg/kg

每只动物体重 g

给药体积 ul

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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制备已知体积和浓度溶液所需的化合物质量
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已知质量的化合物在一定体积内形成的溶液的浓度

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体积（起始）

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

OSU-HDAC42 AR42 HDAC-42 AR-42 (S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺 AR 42 935881-37-1

AR42 相关推荐

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注册成功

AR42

OSU-HDAC42,HDAC-42,AR-42,(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺,AR 42

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