GSK2830371

SIGMA/SML1048 - ≥98% (HPLC)

Synonym: (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

CAS Number: 1404456-53-6
Empirical Formula (Hill Notation): C₂₃H₂₉ClN₄O₂S
Molecular Weight: 461.02
Linear Formula: C₂₃H₂₉ClN₄O₂S
Product Type: Chemical

Catalog Number	PKG Qty.	Price


45-SML1048-5MG	5 mg	$132.00 1/EA	Add To Favorites
45-SML1048-25MG	25 mg	$489.00 1/EA	Add To Favorites

This image is provided for informative purposes only and does not represent an actual product label. It should not be used as a substitute for official product labeling.

Properties
Descriptions
Safety Info.
Basic Data

assay	≥98% (HPLC)
color	white to beige
form	powder
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
Quality Level	100
SMILES string	[s]1c(ccc1C(=O)N[C@@H](CC4CCCC4)C(=O)NC3CC3)CNc2c(ncc(c2)Cl)C
solubility	DMSO: 20 mg/mL, clear
storage temp.	2-8°C

Biochem/physiol Actions:	GSK2830371 is an orally active allosteric inhibitor of wild-type p53-induced phosphatase (Wip1).
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 IC₅₀for 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.
Biochem/physiol Actions:	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.
Packaging:	5, 25 mg in glass bottle

RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point(F)	Not applicable
Flash Point(C)	Not applicable

Purity	≥98% (HPLC)
Storage Temp.	2-8°C
UNSPSC	12352200

To Order From a Quote