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Droxinostat

Droxinostat

产品编号 T6481   CAS 99873-43-5
别名: NS 41080, 4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺

Droxinostat (NS 41080) 是HDAC3、HDAC6和HDAC8抑制剂,IC50分别为16.9、2.47和1.46 μM。

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Droxinostat Chemical Structure
Droxinostat, CAS 99873-43-5
规格 价格/CNY 货期 数量
2 mg ¥ 239 现货
5 mg ¥ 415 现货
10 mg ¥ 693 现货
25 mg ¥ 1,460 现货
50 mg ¥ 2,580 现货
100 mg ¥ 3,950 现货
1 mL * 10 mM (in DMSO) ¥ 445 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: Droxinostat (T6481)
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存储 & 溶解度
参考文献
产品描述 Droxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
靶点活性 HDAC6:2.47 μM, HDAC8:1.46 μM
体外活性 Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). [1] In PPC-1 cells cultured in suspension but not adherent conditions, Droxinostat (20 μM–60 μM) sensitizes cells to anoikis by initially activating caspase 8 with subsequent activation of the mitochondrial pathway. Similarly, Droxinostat also sensitizes other cancer cell lines including PC-3, DU-145, T47D, and OVCAR-3, but not LNCaP or MB-MDA-468, to anoikis or CH-11-induced apoptosis. [2] However, the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). [3] In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis. [4]
体内活性 In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. [2]
激酶实验 HDAC Inhibition Assay: HDAC inhibition is assessed using the CycLex HDACs fluorometric assay according to the manufacturer's protocol and using crude nuclear extract from HeLa cells (principally HDAC1 and HDAC2). The relative activity is expressed as (fluorescence intensity of treated samples/fluorescence intensity of controls) × 100
细胞实验 PPC-1 cells (1 × 104) are seeded overnight into 96-well flat-bottomed plates in 100 μL of medium containing 2.5% FCS. The next day, Droxinostat is added. CH-11 antibody (100 ng/mL) is then added and the cells are incubated for 24 hours before assessing cell viability by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) dye reduction assay.(Only for Reference)
别名 NS 41080, 4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺
分子量 243.69
分子式 C11H14ClNO3
CAS No. 99873-43-5

存储

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

溶解度

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

DMSO: 46 mg/mL (188.8 mM)

Ethanol: 46 mg/mL (188.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 4.1036 mL 20.5179 mL 41.0357 mL 102.5894 mL
5 mM 0.8207 mL 4.1036 mL 8.2071 mL 20.5179 mL
10 mM 0.4104 mL 2.0518 mL 4.1036 mL 10.2589 mL
20 mM 0.2052 mL 1.0259 mL 2.0518 mL 5.1295 mL
50 mM 0.0821 mL 0.4104 mL 0.8207 mL 2.0518 mL
100 mM 0.041 mL 0.2052 mL 0.4104 mL 1.0259 mL

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TargetMol Library Books参考文献

1. Schimmer AD, et al. Cancer Res, 2006, 66(4), 2367-2375. 2. Mawji IA, et al. J Natl Cancer Inst, 2007, 99(10), 811-822. 3. Wood TE, et al. Mol Cancer Ther, 2010, 9(1), 246-256. 4. Bijangi-Vishehsaraei K, et al. Mol Cell Biochem, 2010, 342(1-2), 133-142.
[8]-Shogaol L-Cystathionine Gemcitabine elaidate GGTI298 Trifluoroacetate Tubastatin A Hydrochloride Etalocib Cholesteryl Hemisuccinate 2’-OMe-Guanosine

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 抗癌化合物库 染色质修饰分子库 HIF-1化合物库 抗乳腺癌化合物库 已知活性化合物库 抗胰腺癌化合物库 免疫/炎症分子化合物库 细胞重编程化合物库

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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

Droxinostat 99873-43-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC HDAC3 hepatocellular carcinoma (HCC) NS41080 Histone deacetylases cancer inhibit NS-41080 NS 41080 HDAC6 HDAC8 Inhibitor histone deacetylase (HDAC) 4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺 inhibitor

 

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