1597440-03-3
Chemical Structure
(Rac)-BRD0705
- CAS No.: 1597440-03-3
- Formula:C20H23N3O
- Molecular Weight:321.42
IUPAC Name: 4-ethyl-7,7-dimethyl-4-phenyl-1,2,4,6,7,8-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one
InChIKey: NCKLQXXBRWCYMA-UHFFFAOYSA-N
SMILES: O=C1C2=C(N=C3C(C2(CC)C4=CC=CC=C4)=CNN3)CC(C)(C)C1
Biological Activity: (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].
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(Rac)-BRD0705 | (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). | |||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.
Keywords
