BRD0705
Modify Date: 2024-01-08 19:00:30
BRD0705 structure
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Common Name | BRD0705 | ||
|---|---|---|---|---|
| CAS Number | 2056261-41-5 | Molecular Weight | 321.424 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H23N3O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of BRD0705BRD0705 (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. |
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| 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 |
| Molecular Formula | C20H23N3O |
|---|---|
| Molecular Weight | 321.424 |
| Storage condition | -20°C |