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(E/Z)-BIO-acetoxime

Names

[ CAS No. ]:
740841-15-0

[ Name ]:
(E/Z)-BIO-acetoxime

[Synonym ]:
6-bromoindirubin-3'-acetoxime
GSK-3 INHIBITOR X

Biological Activity

[Description]:

(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM)[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

GSK-3α:10 nM (IC50)

GSK-3β:10 nM (IC50)

Cdk5/p25:2.4 μM (IC50)

CDK2/cyclinA:4.3 μM (IC50)

CDK1/cyclinB:63 μM (IC50)


[In Vitro]

E/Z)-BIO-acetoxime (compound 13) shows more than 200-flod selectivity for GSK-3α/β over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B, with IC50s of 0.01, 2.4, 4.3 and 63 μM, respectively[1].

[References]

[1]. Meijer L, et, al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H12BrN3O3

[ Molecular Weight ]:
398.21000

[ Exact Mass ]:
397.00600

[ PSA ]:
79.79000

[ LogP ]:
3.78120

Related Compounds