GSK 2830371

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Cat.No. 5140 - GSK 2830371 | C23H29ClN4O2S | CAS No. 1404456-53-6
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)
Literature (1)

Biological Activity

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

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

M. Wt 461.02
Formula C23H29ClN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1404456-53-6
PubChem ID 70983932
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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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 are publications that support the biological activity of the product.

Gilmartin et al (2014) Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 10 181 PMID: 24390428

Esfandiari et al (2016) 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. 15 379 PMID: 26832796

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