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GSK 2830371

GSK 2830371 Basic information
Product Name:GSK 2830371
Synonyms:5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide;GSK 2830371;5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide;(S)-5-((5-chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide;2-Thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-;GSK 2830371 USP/EP/BP;GSK 2830371 (S)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino) -1-oxopropan-2-yl)thiophene-2-carboxamide
CAS:1404456-53-6
MF:C23H29ClN4O2S
MW:461.02
EINECS:
Product Categories:Inhibitors
Mol File:1404456-53-6.mol
GSK 2830371 Structure
GSK 2830371 Chemical Properties
Boiling point 704.1±60.0 °C(Predicted)
density 1.30±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: soluble20mg/mL, clear
form powder
pka13.29±0.46(Predicted)
color white to beige
Safety Information
WGK Germany 3
MSDS Information
GSK 2830371 Usage And Synthesis
UsesGSK 2830371 is used in biological studies as allosteric Wip1(wild-type p54-induced phosphatase) inhibition through flap-subdomain interaction.
Biochem/physiol ActionsGSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1, also known as PPM1D/ PP2Cδ), an oncogenic type 2C serine/threonine phosphatase that negatively regulates key proteins in the DNA damage–response pathway. GSK2830371 is selective for Wip1 with an IC50 of 6 nM against Wip1 compared to >10 μM IC50 for PPM1A & PPM1K, and >30 μM IC50 for 22 other phosphatases tested. GSK2830371 is believed to interact with the flap subdomain located near the Wip1 catalytic site, a feature that distinguishes Wip1 from other members of the protein phosphatase 2C (PP2C) family. GSK2830371 increased phosphorylation of Wip1 substrates and caused growth inhibition in both hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53.
storageStore at -20°C
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