BRD0209 是一种有效、选择性和双重的 GSK3α/β 抑制剂 (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM)。BRD0209 还是一种可逆的 ATP 竞争性抑制剂,具有快关动力学 (Ki 分别为 4.2 nM)。BRD0209 是一种三环吡唑并四氢喹啉酮化合物。BRD0209 具有研究心境障碍疾病的潜力。
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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 pyrazolotetradroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases[1].
[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.
DMNPE-caged ATP diammonium salt
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