BRD5648

Names

[ CAS No. ]:
2056261-42-6

[ Name ]:
BRD5648

Biological Activity

[Description]:

BRD5648 ((R)-BRD0705) is an inactive (R)-enantiomer 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]:

Research Areas >> Others

Signaling Pathways >> Others >> Others

[In Vitro]

BRD5648, the inactive enantiomer of BRD0705, does not induce changes in enzyme phosphorylation or total β-catenin protein stabilization[1].

[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]. 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₃N₃O

[ Molecular Weight ]:
321.42

Related Compounds

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