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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-GSK-3-BRD0705
BRD0705

Chemical Structure : BRD0705

CAS No.: 2056261-41-5

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BRD0705 (BRD-0705, BRD 0705)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 321.424
分子式 C20H23N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

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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