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Chemical Structure : BRD0705
CAS No.: 2056261-41-5
Catalog No.: PC-63311Not For Human Use, Lab Use Only.
BRD0705 is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM).
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| 10 mg | $458 | In stock | |
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BRD0705 (BRD-0705) is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM).
BRD0705 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).
BRD0705 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.
BRD0705 impairs leukemia initiation and prolongs survival in AML mouse models.
| M.Wt | 321.424 | |
| Formula | C20H23N3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-4-ethyl-7,7-dimethyl-4-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one |
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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.
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