| Name | BRD0705 |
| Description | BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM). |
| In vitro | 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 (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. 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. |
| In vivo | In AML mouse models, BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 300 mg/mL (933.36 mM), Sonication is recommended.
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| Keywords | β-catenin | Glycogen synthase kinase 3 | leukemia | Acute | survival | inhibit | Inhibitor | oral | myeloid | Glycogen synthase kinase-3 | bioavailability | BRD-0705 | BRD 0705 | BRD0705 | GSK-3 | kinase |
| Inhibitors Related | PHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | CHIR-99021 HCl | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Liver Cancer Compound Library |
United States
