GSK2830371, Catalog: 2578

Alternate Name GSK-2830371

Appearance Off-white to pale yellow solid

CAS # 1404456-53-6 

Molecular Formula C₂₃H₂₉CN₄O₂S

Molecular Weight 461.02

Purity ≥ 98% by HPLC

Solubility DMSO

SMILES CC1=C(NCC2=CC=C(C(N[C@@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)C=C(Cl)C=N1

InChi InChI=1S/C23H29ClN4O2S/c1-14-19(11-16(24)12-25-14)26-13-18-8-9-21(31-18)23(30)28-20(10-15-4-2-3-5-15)22(29)27-17-6-7-17/h8-9,11-12,15,17,20,26H,2-7,10,13H2,1H3,(H,27,29)(H,28,30)/t20-/m0/s1

InChi Key IVDUVEGCMXCMSO-FQEVSTJZSA-N

Storage Conditions -20°C

Shipping Conditions Gel Pack

USAGE For Research Use Only! Not For Use in Humans.

Handling Do not take it internally. Wear a glove and mask when handling the product. Protect from air, light and moisture.

GSK2830371 is an allosteric Wip1 (Wild type p53-induced phosphatase) inhibitor (IC₅₀ of 6 nM). It binds to a flap subdomain that regulates Wip1's enzymatic activity and substrate recognition. Due to lack of this domain in other phosphatases, its binding to GSK2830371 results in a selective and potent inhibition of Wip1. Treatment of tumor cells with the inhibitor 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.