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Cdk5 inhibitor 25-106

Chemical Structure : Cdk5 inhibitor 25-106

CAS No.:

Cdk5 inhibitor 25-106 (Compound 25-106)

Catalog No.: PC-47009Not For Human Use, Lab Use Only.

Cdk5 inhibitor 25-106 is a potent, brain-penetrant inhibitor of Cdk5/p35 activity with IC50 of 178 nM.

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    Biological Activity

    Cdk5 inhibitor 25-106 is a potent, brain-penetrant inhibitor of Cdk5/p35 activity with IC50 of 178 nM.
    Cdk5 inhibitor 25-106 demonstrated similar inhibition against highly homologous Cdk2/Cyclin E (IC50=149 nM), and weak inhibition against CDK9/Cyclin T1 (IC50=5710 nM) in in vitro selectivity assays.
    25-106 significantly reduced phospho-Ser549 synapsin I levels in the striatum 2 h after I.V. injection.
    25-106 inhibits Cdk5 activity in vivo and displays high potency for inhibition in vitro.
    25-106 (50 mg/kg) displayed an increased latency to suspend immobility and displayed a reduction in total immobility time as compared to vehicle-injected mice, modulated behavioral phenotypes linked to Cdk5 through previous characterizations of conditional knockout mice.

    Physicochemical Properties

    M.Wt 345.399
    Formula C18H23N3O4
    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

    N-(5-cyclobutyl-1H-pyrazol-3-yl)-2-(3,4,5-trimethoxyphenyl)acetamide

    References

    1. Umfress A, et al. Front Pharmacol. 2022 May 12;13:863762.

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