GSK 2830371
Chemical Name: 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Chemical inhibition of wild-type p53-induced phosphatase 1 (WIP1/PPM1D) by GSK2830371 potentiates the sensitivity to MDM2 inhibitors in a p53-dependent manner.
Esfandiari et al.
Mol.Cancer Ther., 2016;15:379 -
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin et al.
Nat.Chem.Biol., 2014;10:181
Product Datasheets
Citation for GSK 2830371
The citations listed below are publications that use Tocris products. Selected citations for GSK 2830371 include:
1 Citation: Showing 1 - 1
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Parainfluenza Virus Infection Sensitizes Cancer Cells to DNA-Damaging Agents: Implications for Oncolytic Virus Therapy.
Authors: Griffith D Et al.
J Virol 2018;92
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