化合物BSJ-03-123 T5395

Product Introduction
Bioactivity


英文名: BSJ-03-123

描述: BSJ-03-123是一种有效的 CDK6 选择性小分子降解剂，是由 Cereblon 配体和 CDK 配体相连的 PROTAC。

细胞实验: 4x10^6 MV4-11 CRBN-/- cells were treated for 3 h with 20 μM palbociclib, BSJ-03-123 or vehicle. 1x10^6 cells were spun down at 500 x g for 5 min, and the supernatant removed. Pellets were incubated at 46, 49, 52 or 55°C for 3 min followed by 3 min incubation at room temperature. 30 μl of lysis buffer (20 mM Tris-HCl pH 8.0, 120 mM NaCl, 0.5% NP-40, protease inhibitors) were added and cells lysed by 3 rounds of snap freezing and thawing. Denatured proteins were removed by 20 min centrifugation at 14.000 x g at 4°C and supernatants analyzed by Western Blotting.

体外活性: BSJ-03-123 induced rapid, dose-dependent ternary complex formation with CDK6 and CRBN, but not with CDK4 and CRBN. Ternary complex formation was prevented by blocking binding sites on CDK6 or CRBN via pretreatment with palbo or lenalidomide.

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 115 mg/mL (122.73 mM)
H2O : Insoluble


关键字: Inhibitor | CDK | PROTACs | Cyclin dependent kinase | inhibit | BSJ-03-123 | BSJ03123 | BSJ 03 123

相关产品: Cucurbitacin E | Aloisine B | GW297361 | MBM-55 | ML141 | Trilaciclib hydrochloride | AM5992 | AZD4573 | NSC23005 | Cdc7-IN-1

相关库: Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途