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BRD0209 (BRD 0209)

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BRD0209 (BRD 0209) Basic information

Product Name:
BRD0209 (BRD 0209)
Synonyms:
  • BRD0209 (BRD 0209)
  • BRD0209
  • 5H-Pyrazolo[3,4-b]quinolin-5-one, 3-cyclopropyl-1,2,4,6,7,8-hexahydro-4,7,7-trimethyl-4-phenyl-, (4S)-
  • (S)-3-Cyclopropyl-4,7,7-trimethyl-4-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one
  • BRD0209/(S)-3-Cyclopropyl-4,7,7-trimethyl-4-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one
  • BRD0209, 10 mM in DMSO
  • (4S)-3-cyclopropyl-4,7,7-trimethyl-4-phenyl-2,6,8,9-tetrahydropyrazolo[3,4-b]quinolin-5-one
CAS:
1597439-87-6
MF:
C22H25N3O
MW:
347.45
Mol File:
1597439-87-6.mol
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BRD0209 (BRD 0209) Chemical Properties

form 
Solid
color 
Light yellow to yellow
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BRD0209 (BRD 0209) Usage And Synthesis

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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