| Identification | Back Directory | [Name]
BRD0209
(BRD 0209) | [CAS]
1597439-87-6 | [Synonyms]
BRD0209
BRD0209
(BRD 0209)
5H-Pyrazolo[3,4-b]quinolin-5-one, 3-cyclopropyl-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)- | [Molecular Formula]
C22H25N3O | [MOL File]
1597439-87-6.mol | [Molecular Weight]
347.45 |
| Hazard Information | Back Directory | [Description]
BRD0209 is a highly selective and potent GSK3 inhibitor. BRD0209 demonstrates in vivo efficacy in a dopaminergic signaling paradigm modeling mood-related disorders. The mood stabilizer lithium, the first-line treatment for bipolar disorder, is hypothesized to exert its effects through direct inhibition of glycogen synthase kinase 3 (GSK3). | [Uses]
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases[1]. | [References]
[1] Wagner FF, et al. Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects. ACS Chem Biol. 2016;11(7):1952-1963. DOI:10.1021/acschembio.6b00306 |
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