Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50: 515 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 253.00 | |
2 mg | In stock | $ 353.00 | |
5 mg | In stock | $ 538.00 | |
10 mg | In stock | $ 778.00 | |
25 mg | In stock | $ 1,180.00 | |
50 mg | In stock | $ 1,620.00 | |
100 mg | In stock | $ 2,180.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 585.00 |
Description | BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50: 515 nM). |
Targets&IC50 | GSK-3α:4.8 μM (Kd), GSK-3α:66 nM, GSK-3β (WT):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. |
Molecular Weight | 321.42 |
Formula | C20H23N3O |
CAS No. | 2056261-41-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 300 mg/mL (933.36 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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BRD0705 2056261-41-5 PI3K/Akt/mTOR signaling Stem Cells GSK-3 β-catenin Glycogen synthase kinase 3 leukemia Acute survival inhibit Inhibitor oral myeloid Glycogen synthase kinase-3 bioavailability BRD-0705 BRD 0705 kinase inhibitor