GSK 2830371

Cat. No. 5140

GSK 2830371 C23H29ClN4O2S [1404456-53-6]

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Chemical Name: 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide

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. Orally bioavailable.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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Keywords: GSK 2830371, supplier, GSK2830371, potent, selective, allosteric, inhibitors, inhibits, wip1, phosphatases, antitumor, orally, bioavailable, Tocris Bioscience, Protein Ser/Thr Phosphatases Inhibitor products

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