(Rac)-BRD0705 是 BRD0705 的低活性外消旋体，BRD0705 是一种有效的，具有旁系选择性和口服活性的 GSK3α 抑制剂，IC50 为 66 nM，Kd 为 4.8 μM。BRD0705 与 GSK3β (IC50 为 515 nM) 相比，对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于治疗急性髓细胞性白血病。
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used to treat acute myeloid leukemia (AML)[1][2].
[1]. Wagner FF, et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. [2]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.
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