GSK 2830371

Catalog # Availability Size / Price Qty
5140/10
5140/50
Cat.No. 5140 - GSK 2830371 | C23H29ClN4O2S | CAS No. 1404456-53-6
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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%

Product Details
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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.

Technical Data

M.Wt:
461.02
Formula:
C23H29ClN4O2S
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1404456-53-6

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

Licensing Caveats:
Sold for research purposes only under agreement from GlaxoSmithKline

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