Key Specifications Table
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|5.30306.0001||Glass bottle||10 mg||
|Overview||A cell-permeable, orally available pyridinylaminomethylthienylcarboxamide compound that acts as a potent, allosteric, non-competitive, and reversible inhibitor of wild-type p53-induced phosphatase (Wip1; IC50 = 6 nM for dephosphorylation of fluorescein diphosphate by Wip1 (2-240) and 13 nM for phospho-p38 MAP kinase (Thr180)). Does not affect the activity of 21 other phosphatases studied (IC50 ≥ 30 µM). Binds to the flap region in close proximity to Wip1 catalytic site and impairs ubiquitin-mediated degradation of Wip1. Co-treatment of cells with MG-132 (Cat. No. 474790) reverses the reduction in Wip1 levels in cells. Enhances phosphorylation of Chk2 (Thr68), p53 (Ser15), H2AX (Ser139), and ATM (Ser1981) and upregulates the levels of p21/WAF1 in various tumor cells. Shown to block the growth of hematopoietic tumor cell lines and Wip1-amplified breast tumor cells harboring wild-type TP53, but does not affect BT474 cells carrying mutant p53 and amplified Wip1. Due to its short half life and reversible action, a sustained inhibition is warranted to block tumor growth. Reduces the growth of DOHH2 lymphoma tumor xenografts in mice (~150 mg/kg, p.o. bid or tid).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
|Synonyms||(S)-5-((5-Chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide, PP2Cδ Inhibitor II, Wip1 Inhibitor II, WT-53-Induced Phosphatase Inhibitor; GSK 2830371|
|References||Gilmartin, A.G., et al. 2014. Nature Chem. Biol. 10, 181.|
|Form||Light yellow powder|
|Primary Target IC<sub>50</sub>||6 nM for dephosphorylation of fluorescein diphosphate by Wip1 (2-240) and 13 nM for phospho-p38 MAP kinase (Thr180)|
|Purity||≥97% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Global Trade Identification Number|
PPM1D Phosphatase Inhibitor II, GSK2830371 - Calbiochem SDS
|Gilmartin, A.G., et al. 2014. Nature Chem. Biol. 10, 181.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.