A potent and selective inhibitor of Wip1 (IC50 = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable

GSK2830371 – 25 mg

Brand:
Cayman
CAS:
1404456-53-6
Storage:
-20
UN-No:
Non-Hazardous - /

The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer.{27983,27982} GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).{27981} It displays selectivity for Wip1 over 21 other phosphatases.{27981} GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.{27981} This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.{27981}  

 

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Description

A potent and selective inhibitor of Wip1 (IC50 = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice

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

Synonyms: 

Molecular weight: 461

CAS: 1404456-53-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling

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