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BRD0705

Cat. No. M10530

All AbMole products are for research use only, cannot be used for human consumption.

BRD0705 Structure
Size Price Availability Quantity
5mg USD 600 In stock
10mg USD 950 In stock
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Biological Activity

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 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). BRD0705 treatments on U937 cells impairs GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation.

In vivo, BRD0705 (30 mg/kg; oral gavage; twice daily) treatment on NSG mice impairs leukemia initiation and prolongs survival in AML mouse models.

Chemical Information
Molecular Weight 321.42
Formula C20H23N3O
CAS Number 2056261-41-5
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Souvik Dey, et al. FASEB J. Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs

[2] Laura Hinze, et al. Cancer Cell. Synthetic Lethality of Wnt Pathway Activation and Asparaginase in Drug-Resistant Acute Leukemias

[3] Florence F Wagner, et al. Sci Transl Med. Exploiting an Asp-Glu switch in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia

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Abmole Inhibitor Catalog




Keywords: BRD0705 supplier, GSK-3, inhibitors, activators

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