| Name | BRD3731 |
|---|---|
| Synonyms |
(4R)-3-(2,2-dimethylpropyl)-4,7,7-trimethyl-4-phenyl-2,6,8,9-tetrahydropyrazolo[3,4-b]quinolin-5-one
(R)-BRD3731 5H-Pyrazolo[3,4-b]quinolin-5-one, 3-(2,2-dimethylpropyl)-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4R) BRD3731 (BRD-3731 |
| Description | 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. |
|---|---|
| References | References 1. Wagner FF, et al. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. View Related Products by Target GSK-3 |
| Molecular Formula | C24H31N3O |
|---|---|
| Molecular Weight | 377.532 |