BSJ-03-123

产品编号 T5395   CAS T5395

BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.

BSJ-03-123结构式
BSJ-03-123 , CAS T5395
规格 库存 价格/RMB 数量
1 mg 上海现货 998.00
5 mg 上海现货 2218.00
10 mg 上海现货 3106.00
50 mg 上海现货 6699.00
1 mL * 10 mM (in DMSO) 上海现货 2800.00
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生物活性
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存储 & 溶解度
产品描述 BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.
靶点活性 CDK6,  
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.
Cell Research
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.
别名
纯度 99.38%
分子量 937.01
分子式 C48H57N9O11
CAS No. T5395

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

DMSO: 115 mg/mL (122.73 mM)

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

文献引用

参考文献
1. Brand M, et al. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9.

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