Product Name: GSK-2830371 Request
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GSK2830371 is a orally active, allosteric inhibitor of Wip1 phosphatase with IC50 of 6 nM.
in vitro: GSK2830371 potently inhibited Wip1 (2-420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC50 values of 6 nM and 13 nM, respectively. GSK2830371 showed no inhibition of any of the 21 additional phosphatases tested, confirming the selective inhibition of Wip1 phosphatase. In the PPM1D-amplified MCF7 breast carcinoma cells, treatment with GSK2830371 increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1 amplified, p53 wild type) with GSK2830371 caused concentration-dependent effects in cell growth assays. Treatment with GSK2830371 would cause increase in phospho-substrates Chk2(T68) and p53(S15) only in the presence of functional ATM kinase activity . in vivo: GSK2830371 for testing on the basis of its biochemical potency and oral bioavailability in mice. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK2830371 inhibited the growth of DOHH2 tumor xenografts by 41% and 68%, respectively (Fig. 6b). Comparable tumor growth inhibition was observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 2 years.