An inhibitor of GSK3
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CAY10796

Item No. 21190

Technical Information
Formal Name
N-(5-methyl-1H-pyrazol-3-yl)-2-phenyl-4-quinazolinamine
CAS Number
404828-14-4
Molecular Formula
C18H15N5
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 0.25 mg/mlDMSO: 0.15 mg/ml
λmax
210, 249, 331 nm
SMILES
CC1=CC(NC2=NC(C3=CC=CC=C3)=NC4=C2C=CC=C4)=NN1
InChi Code
InChI=1S/C18H15N5/c1-12-11-16(23-22-12)20-18-14-9-5-6-10-15(14)19-17(21-18)13-7-3-2-4-8-13/h2-11H,1H3,(H2,19,20,21,22,23)
InChi Key
JYCUVOXSZBECAY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CAY10796 is an aminopyrazole ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3), with 34% inhibition when used at a concentration of 2.5 µM.1 It inhibits androgen receptor transactivation in 22Rv1, LNCaP, and LNCaP-SSR cell lines in a dose-dependent manner. It promotes nuclear export of the androgen receptor and decreases translocation to the nucleus in PC3 and PCa prostate cancer cells, respectively.1,2 In HEK293 cells expressing the rat Nav1.2 channel, pretreatment with CAY10796 dose-dependently potentiates peak current densities.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rinnab, L., Schütz, S.V., Diesch, J., et alInhibition of glycogen synthase kinase-3 in androgen-responsive prostate cancer cell lines: are GSK inhibitors therapeutically useful? Neoplasia 10(6), 624-634 (2008).

    2. Schütz, S.V., Cronauer, M.V., and Rinnab, L. Inhibition of glycogen synthase kinase-3β promotes nuclear export of the androgen receptor through a CRM1-dependent mechanism in prostate cancer cell lines. J. Cell. Biochem. 109(6), 1192-1200 (2010).

    3. James, T.F., Nenov, M.N., Wildburger, N.C., et alThe Nav1.2 channel is regulated by GSK3. Biochim. Biophys. Acta 1850(4), 832-844 (2015).