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Plek2 inhibitor NUP-17d

Chemical Structure : Plek2 inhibitor NUP-17d

CAS No.: 950240-00-3

Plek2 inhibitor NUP-17d

Catalog No.: PC-49703Not For Human Use, Lab Use Only.

Plek2 inhibitor NUP-17d is a specific small molecule inhibitor of Pleckstrin-2 (Plek2), binds to Plek2 and Plek2-DEP with high affinity (ITC KD=109 and 350 nM, respectively).

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    Biological Activity

    Plek2 inhibitor NUP-17d is a specific small molecule inhibitor of Pleckstrin-2 (Plek2), binds to Plek2 and Plek2-DEP with high affinity (ITC KD=109 and 350 nM, respectively).
    NUP-17d has IC50 of 7.8 µM in the erythroid in vitro proliferation assay.
    NUP-17d also significantly inhibited enucleation and differentiation (at higher dosage) of the cultured erythroid cells and induced apoptosis.
    NUP-17d is specific for Plek2, showed no inhibitory effect when Plek2 was acutely depleted by shRNA.
    NUP-17d dramatically reverted lamellipodia in Plek2 overexpressed cells (Cos-7 cells), blocked Plek2-mediated Akt activation, induceed a confirmation change of Plek2 protein, which leads to Akt dissociation from the lipid-Plek2 complex and instability.
    NUP-17d (25 mg/kg, 10% DMSO, 2% ethanol, 2% TWEEN80 and 86% 0.5% captisol) significantly reduced EPO-induced leukocytosis, reticulocytosis, extramedullary erythropoiesis, and vascular occlusions in the lungs of EPO injection models.
    NUP-17d (25 mg/kg) reduced myeloproliferation in JAK2V617F models.
    NUP-17d (25 mg/kg) demonstrated synergistic effects when combined with Akt inhibitor MK-2206 in human MPN cells.
    Pleckstrin-2 (Plek2) is a downstream target of the JAK2-STAT pathway and overexpressed in patients with myeloproliferative neoplasms (MPNs), Plek2 activates Akt and protects Akt through Hsp72.

    Physicochemical Properties

    M.Wt 397.90
    Formula C22H24ClN3O2
    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

    3-(4-chlorophenyl)-2-hydroxy-1-(1H-indol-3-yl)-3-(4-methylpiperazin-1-yl)propan-1-one

    References

    1. Xu Han, et al. J Clin Invest. 2023 Jan 31;e159638.

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