BRD0705 MedChemExpress (MCE)

Product Name	BRD0705
Synonyms	BRD0705;BRD0705 (BRD-0705
CAS	2056261-41-5
EINECS
Chemical Formula	C20H23N3O
Molecular Weight	321.42
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	BRD0705 BRD0705 MedChemExpress (MCE) HY-116830 2056261-41-5 99.80% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions BRD0705 BRD0705 MedChemExpress (MCE) HY-116830 2056261-41-5 99.80% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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) research. BRD0705 displays excellent selectivity in a penal of 311 kinases, the CDK family of kinases (CDK2, 3 and 5) are next most potently inhibits at values of 6.87 μM, 9.74 μM and 9.20 μM (87-fold, 123-fold and 116-fold selectivity relative to GSK3α)[1]. BRD0705 (10-40 μM 2-24 hours U937 cells) treatment impairs GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation[1]. Using a β-catenin dependent TCF/LEF luciferase reporter assay, the absence of β-catenin induced target activation after treatment with BRD0705 in AML cell lines[1]. BRD0705 impairs AML colony formation in all six tested cell lines, MOLM13, TF-1, U937, MV4-11, HL-60 and NB4, in a concentration-dependent manner, as opposed to BRD3731 which impairs colony formation in TF-1 while increasing colony forming ability in the MV4-11 cell line[1]. BRD0705 (30 mg/kg oral gavage twice daily NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models[1]. GSK3α 66 nM (IC50) GSK3α 4.8 μM (Kd) GSK-3β(WT) 515 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

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