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NRT-870-59

Chemical Structure : NRT-870-59

CAS No.: 2284492-36-8

NRT-870-59 (NRT 870-59)

Catalog No.: PC-73092Not For Human Use, Lab Use Only.

NRT-870-59 is a potent, reversible PTP4A3 inhibitor (IC50=86 nM) with inhibitory specificity for PTP4A3 versus both PTP4A3 A111S mutant and CDC25B.

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    Biological Activity

    NRT-870-59 is a potent, reversible PTP4A3 inhibitor (IC50=86 nM) with inhibitory specificity for PTP4A3 versus both PTP4A3 A111S mutant and CDC25B.
    NRT-870-59 does not inhibit CDC25B and PTP4A3 A111S mutant at 1 uM, and 5- to 6-fold less potent aginst DUSP3.
    NRT-870-59 inhibits PTP4A1, PTP4A2, PTP4A3 mutants C49S, K144I and A106V with IC50 of 133.2, 264.4, 86.0, 332.2, 180.2 and 57.7 nM, respectively.
    NRT-870-59 inhibits cancer cell colony formation, which is required PTP4A3 expression.
    The PTP4A (phosphatase of regenerating liver/PRL) phosphatases are a unique subfamily of protein tyrosine phosphatases (PTPs) comprising three highly homologous members (PTP4A1, PTP4A2, and PTP4A3) with 80% amino acid sequence identity.
    PTP4A3, and to a lesser extent PTP4A1 and PTP4A2, are overexpressed in many types of cancer, promote tumor invasion and dissemination, and contribute to poor patient prognosis.

    Physicochemical Properties

    M.Wt 270.306
    Formula C14H10N2O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    7-imino-5-methyl-2-phenylthieno[3,2-c]pyridine-4,6(5H,7H)-dione

    References

    1. Lazo JS, et al. J Pharmacol Exp Ther. 2019 Dec;371(3):652-662

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