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Chemical Structure : GSK2830371
CAS No.: 1404456-53-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $78 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $238 | In stock | |
| 100 mg | $378 | In stock | |
| 250 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 461.0 | |
| Formula | C23H29ClN4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide |
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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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