产品说明书

BSJ-4-116

Print
Chemical Structure| 2519823-34-6 同义名 : -
CAS号 : 2519823-34-6
货号 : A1472916
分子式 : C40H49ClN8O8S
纯度 : 98+%
分子量 : 837.384
MDL号 : MFCD34186973
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(298.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 BSJ-4-116 is a PROTAC comprising ligands for Cereblon and CDK. It serves as a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes by inducing premature termination of transcription, primarily through increased poly(adenylation). It demonstrates robust antiproliferative effects, both alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.19mL

0.24mL

0.12mL

5.97mL

1.19mL

0.60mL

11.94mL

2.39mL

1.19mL
参考文献

[1]Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683.