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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-GSK2830371
GSK2830371

Chemical Structure : GSK2830371

CAS No.: 1404456-53-6

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GSK2830371 (GSK-2830371)

货号: PC-38476Not For Human Use, Lab Use Only.

GSK2830371 (GSK 2830371) is a potent, selective orally active, allosteric inhibitor of Wip1 phosphatase (PPM1D) with IC50 of 6 nM, inhibits endogenous substrates phospho-p38 MAPK (T180) with IC50 of 13 nM.

规格 价格 库存 数量
10 mg ￥580 In stock
25 mg ￥980 In stock
50 mg ￥1580 In stock
100 mg ￥2580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2830371 (GSK 2830371) is a potent, selective orally active, allosteric inhibitor of Wip1 phosphatase (PPM1D) with IC50 of 6 nM, inhibits endogenous substrates phospho-p38 MAPK (T180) with IC50 of 13 nM.
GSK2830371 (GSK 2830371) showed no inhibition of any of the 21 additional phosphatases tested.
GSK2830371 increases phosphorylation of Wip1 substrates and causes growth inhibition in both hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53.
GSK2830371 (GSK 2830371) oral dosing at 150 mg/kg BID (twice daily) and TID (thrice daily) inhibited the growth of
DOHH2 tumor xenografts by 41% and 68%, respectively.

物理化学性质&存储条件

分子量 461.0
分子式 C23H29ClN4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide

参考文献

1. Gilmartin AG, et al. Nat Chem Biol. 2014 Mar;10(3):181-7.

2. Richter M, et al. PLoS One. 2015 Feb 6;10(2):e0115635.

3. Esfandiari A, et al. Mol Cancer Ther. 2016 Mar;15(3):379-91.

4. Pechackova S, et al. Oncotarget. 2016 Mar 22;7(12):14458-75.

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