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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.
Sold for research purposes only under agreement from GlaxoSmithKline
Compound Libraries for GSK 2830371
Technical Data for GSK 2830371
|Storage||Store at -20°C|
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 for GSK 2830371
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
References for GSK 2830371
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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Keywords: GSK 2830371, GSK 2830371 supplier, GSK2830371, potent, selective, allosteric, inhibitors, inhibits, wip1, phosphatases, antitumor, orally, bioavailable, Protein, Ser/Thr, Phosphatases, 5140, Tocris Bioscience
1 Citation for GSK 2830371
Citations are publications that use Tocris products. Selected citations for GSK 2830371 include:
Griffith D et al (2018) Parainfluenza Virus Infection Sensitizes Cancer Cells to DNA-Damaging Agents: Implications for Oncolytic Virus Therapy. J Virol 92 PMID: 29343567
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Literature in this Area
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