GSK 2830371

Name: GSK 2830371
Brand: Tocris Bioscience
SKU: 5140

Tocris Bioscience, part of Bio-Techne | Catalog # 5140

Citations (5)

COA / SDS

Potent and selective allosteric inhibitor of Wip1 phosphatase

Key Product Details

Description:	Potent and selective allosteric inhibitor of Wip1 phosphatase
Chemical Name:	5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	461.02

View Full Technical Details for GSK 2830371

Technical Data
Citations

Biological Activity for GSK 2830371

GSK 2830371 is a potent and selective allosteric inhibitor of Wip1 phosphatase (IC₅₀ = 6 nM). Exhibits selectivity for Wip1 over 21 other phosphatases. Increases phosphorylation of Wip1 substrates, including p53, Chk2, H2AX and ATM. Attenuates tumor cell growth in a variety of lymphoid cell lines. Also inhibits lymphoma xenograft growth in vivo. Potentiates growth inhibitory effects of MDM2 inhibition in cancer cell lines in a p53-dependent manner. Orally bioavailable.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Compound Libraries for GSK 2830371

GSK 2830371 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2830371

M. Wt	461.02
Formula	C₂₃H₂₉ClN₄O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1404456-53-6
PubChem ID	70983932
InChi Key	IVDUVEGCMXCMSO-FQEVSTJZSA-N
Smiles	ClC1=CC(NCC2=CC=C(C(N[C@H]([C@@](NC4CC4)=O)CC3CCCC3)=O)S2)=C(C)N=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 2830371

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	46.1	100
	ethanol	23.05	50

Preparing Stock Solutions for GSK 2830371

The following data is based on the product molecular weight 461.02.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.17 mL	10.85 mL	21.69 mL
5 mM	0.43 mL	2.17 mL	4.34 mL
10 mM	0.22 mL	1.08 mL	2.17 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

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References for GSK 2830371

References are publications that support the biological activity of the product.

Esfandiari Chemical inhibition of wild-type p53-induced phosphatase 1 (WIP1/PPM1D) by GSK2830371 potentiates the sensitivity to MDM2 inhibitors in a p53-dependent manner. Mol.Cancer Ther. 2016 PMID: 26832796
Gilmartin Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 2014 PMID: 24390428