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BRD3731

Chemical Structure : BRD3731

CAS No.: 2056262-08-7

BRD3731 (BRD-3731;BRD 3731)

Catalog No.: PC-63312Not For Human Use, Lab Use Only.

BRD3731 is a potent, selective GSK3β inhibitor with IC50 of 15 nM, 14-fold selectivity for GSK3β over GSK3α (IC50=215 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BRD3731 is a potent, selective GSK3β inhibitor with IC50 of 15 nM, 14-fold selectivity for GSK3β over GSK3α (IC50=215 nM); displays excellent selectivity in a penal of 311 kinases, displays reduced potency toward the GSK3β mutant (D133E) with IC50 of 53 nM; induces β-catenin stabilization starting at 20 uM in the HL-60 AML cell line, decreases β-catenin S33/37/T41 phosphorylation and induces β-catenin S675 phosphorylation, resulting in increased β-catenin.

Physicochemical Properties

M.Wt 377.532
Formula C24H31N3O
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

(R)-4,7,7-trimethyl-3-neopentyl-4-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one

References

1. Wagner FF, et al. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460.

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