| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (15.56 mM), Sonication is recommended.
DMSO : 300 mg/mL (933.36 mM), Sonication is recommended.
|
| Keywords | β-catenin | survival | oral | myeloid | leukemia | kinase | Inhibitor | inhibit | GSK-3β(WT) | GSK-3α | GSK3α | GSK-3 | GSK3 | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | BRD-0705 | BRD0705 | BRD 0705 | bioavailability | Acute |
| Inhibitors Related | Cromolyn sodium | 4-Methyl-6-Methoxycoumarin | Indazole | GSK 3 Inhibitor IX | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | Ethyl linoleate | Ginsenoside Rg2 | GSK-3 Inhibitor 5 | (E/Z)-10-Hydroxy-2-decenoic acid | ROCK-IN-5 |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Oxidation-Reduction Compound Library |
United States
