BRD0705 is a first-in-class, paralog selective GSK3α inhibitor with an IC50 value of 0.066 μM. BRD0705 induced differentiation, reduced transcriptional programs of stemness and impaired colony formation in AML cell lines and primary patient samples without affecting normal hematopoietic cell growth. Importantly, BRD0705 did not induce β-catenin stabilization or nuclear translocation at concentrations efficacious in multiple mouse models of AML, resulting in leukemia initiation impairment and prolonged survival.

The negative control BRD5648 is available as Axon 3153. The racemic mixture of both enantiomers is available as Axon 3154.

KEYWORDS: BRD0705 | supplier | GSK3α inhibitor | BRD 0705 | BRD-0705 | CAS [2056261-41-5] | Non Selective (Phosphorylation Substrates) | GSK-3 | Inhibitor | Enzymes | AML