NSC 95397: Potent, Selective Irreversible Inhibitor of Cdc25 Dual Specificity Phosphatases

Now Available from Sigma-RBI

Prod. No. N 1786

Dual specificity protein phosphatases uniquely dephosphorylate both phosphoserines/threonines and phosphotyrosines on the same protein substrate. They regulate intracellular signaling through mitogen activated and stress activated kinases, oncogenesis and cell cycle progression through G1/S and G2/M checkpoints. The Cdc25 phosphatases have been implicated in cancer and Alzheimer’s disease.^1,2 Three Cdc25 homologs exist in humans and are referred to as Cdc25A, Cdc25B, and Cdc25C. They are expressed and activated at different times during the cell cycle. Until recently, potent and selective inhibitors of this enzyme class were not available.

Sigma-RBI is pleased to introduce NSC 95397 as a potent and selective irreversible inhibitor of Cdc25 dual specificity phosphatase:

• Inhibits in vitro oncogenic, full-length, recombinant human CdC25B with IC50 <500 nM.³
• Displays mixed inhibition kinetics with in vitro Ki values for Cdc25A, -B, and -C of 32, 96, and 40 nM, respectively.³
• 125- to 180-fold more selective for Cdc25A than VH1-group of dual specificity phosphatases or protein tyrosine phosphatase PTP1B, respectively.³
• Significantly inhibits in vitro growth of human and murine carcinoma cells and blocks G2/M cell cycle phase transition.³

Physical Description Solubility Molecular Formula Formula Weight Sizes

An orange solid Soluble in DMSO at 16 mg/ml C14H14O4S2 310.39 5 mg, 25 mg

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