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CAS No. : 2056261-41-5
MCE 国际站:BRD0705
产品活性:BRD0705 是一种有效的,具有旁系选择性和口服活性的 GSK3α 抑制剂,IC50 为 66 nM,Kd 为 4.8 μM。 BRD0705 与 GSK3β (IC50 为 515 nM) 相比,对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病的研究。
研究领域:PI3K/Akt/mTOR | Stem Cell/Wnt
作用靶点:GSK-3
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.
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.
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: BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models.
相关产品:Bioactive Compound Library Plus | BRD5648 | AR-A014418 | GSK-3β inhibitor 3 | SAR502250 | GSK 3 Inhibitor IX | K00546 | GSK-3β inhibitor 10 | DIF-3 | GSK3-IN-2 | RGB-286638 | Laduviglusib (GMP) | ROCK-IN-5 | Indirubin-3′-oxime | GSK-3β inhibitor 2 | Bikinin | Alsterpaullone | GSK3 Substrate, α, β subunit | Indirubin-3'-monoxime | GSK-3 Inhibitor XIII | GSK-3β inhibitor 7 | Aloisine A | Aloisine RP106 | GSK-3β inhibitor 11 | AChE/BACE1/GSK3β-IN-1 | 7BIO | 5-Iodo-indirubin-3'-monoxime | 6-Me-ATP trisodium | 3F8
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