GSK 2830371
- CAS No.
- 1404456-53-6
- Chemical Name:
- GSK 2830371
- Synonyms
- GSK 2830371;GSK 2830371 USP/EP/BP;(S)-5-((5-chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide;5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide;5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide;2-Thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-;GSK 2830371 (S)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino) -1-oxopropan-2-yl)thiophene-2-carboxamide
- CBNumber:
- CB72682001
- Molecular Formula:
- C23H29ClN4O2S
- Molecular Weight:
- 461.02
- MOL File:
- 1404456-53-6.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/6/30 15:45:59
GSK 2830371 price More Price(2)
GSK 2830371 Chemical Properties,Uses,Production
Uses
GSK 2830371 is used in biological studies as allosteric Wip1(wild-type p54-induced phosphatase) inhibition through flap-subdomain interaction.
Biochem/physiol Actions
GSK2830371 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.
GSK 2830371 Preparation Products And Raw materials
GSK 2830371 Suppliers
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