Description: BRD0705 HCl is a novel, potent, paralog selective and orally bioactive glycogen synthase kinase 3α (GSK3α) inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. GSK3 is a key regulatory kinase in the wingless-type MMTV integration site family (WNT) pathway, is a therapeutic target of interest in many diseases. The GSK3α-selective compound BRD0705 inhibits kinase function and does not stabilize β-catenin, mitigating potential neoplastic concerns. BRD0705 induces myeloid differentiation and impairs colony formation in AML cells, with no apparent effect on normal hematopoietic cells. Moreover, BRD0705 impairs leukemia initiation and prolongs survival in AML mouse models. These studies demonstrate feasibility of paralog-selective GSK3α inhibition, offering a promising therapeutic approach in AML.

Referenes:

[1]. 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.

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[3]. /5/528.1

纯度：≥98%

CAS：2056261-41-5 (free base)