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(Rac)-BRD0705

Names

[ CAS No. ]:
1597440-03-3

[ Name ]:
(Rac)-BRD0705

Biological Activity

[Description]:

(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 for acute myeloid leukemia (AML)[1][2].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H23N3O

[ Molecular Weight ]:
321.42

Related Compounds