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SML1048

Sigma-Aldrich

GSK2830371

≥98% (HPLC)

Synonym(s):

(S)-5-(((5-Chloro-2-methylpyridin-3-yl)amino)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-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide

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About This Item

Empirical Formula (Hill Notation):
C23H29ClN4O2S
CAS Number:
Molecular Weight:
461.02
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

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

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.
GSK2830371 prevents the development of neuroblastoma by stimulating cell death mediated by Chk2 (checkpoint kinase 2)/p53. In neuroblastoma (NB) cell lines, GSK2830371 increased the cytotoxicity stimulated by doxorubicin- (Dox) and etoposide- (VP-16). It also blocks the capability of a subset of NB cells in multiplication and colony formation.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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Zhenghu Chen et al.
Scientific reports, 6, 38011-38011 (2016-12-20)
Neuroblastoma (NB) is the most common extracranial tumor in children. Unlike in most adult tumors, tumor suppressor protein 53 (p53) mutations occur with a relatively low frequency in NB and the downstream function of p53 is intact in NB cell

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