2056261-41-5

2056261-41-5 structure

Name: BRD0705
Chemical Name: BRD0705
CAS Number: 2056261-41-5
Molecular Formula: C₂₀H₂₃N₃O
Molecular Weight: 321.424
Catalog: Signaling Pathways PI3K/Akt/mTOR GSK-3
Create Date: 2020-01-20 09:10:56
Modify Date: 2024-01-08 19:00:30
BRD0705 (BRD-0705) is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM); displays excellent selectivity in a penal of 311 kinases, the CDK family of CDK2, CDK3 and CDK5) are most potently inhibited with IC50 of 6.87, 9.74 and 9.20 uM (87-, 123-, and 116-fold selectivity relative to GSK3α); inhibits GSK3α kinase function, impairs GSK3α Tyr279 phosphorylation in a time- and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation, and does not stabilize β-catenin, induces myeloid differentiation and impairs colony formation in AML cells, with no apparent effect on normal hematopoietic cells; impairs leukemia initiation and prolongs survival in AML mouse models.

Name	BRD0705

Description	BRD0705 (BRD-0705) is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM); displays excellent selectivity in a penal of 311 kinases, the CDK family of CDK2, CDK3 and CDK5) are most potently inhibited with IC50 of 6.87, 9.74 and 9.20 uM (87-, 123-, and 116-fold selectivity relative to GSK3α); inhibits GSK3α kinase function, impairs GSK3α Tyr279 phosphorylation in a time- and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation, and does not stabilize β-catenin, induces myeloid differentiation and impairs colony formation in AML cells, with no apparent effect on normal hematopoietic cells; impairs leukemia initiation and prolongs survival in AML mouse models.
References	References 1. Wagner FF, et al. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. 2. Cancer Discov. 2018 Mar 16. doi: 10.1158/2159-8290.CD-RW2018-046. View Related Products by Target GSK-3