货号	规格	价格	上海	北京	珠海	重庆	武汉
S89250-5mg买3赠1	98.90%	￥720.00 S89250-5mg ￥720.00 现货（买3赠1）	5 5	-	-	-	-
S89250-10mg买3赠1	98.90%	￥900.00 S89250-10mg ￥900.00 现货（买3赠1）	6 6	-	-	-	-
S89250-25mg买3赠1	98.90%	￥1260.00 S89250-25mg ￥1260.00 现货（买3赠1）	5 5	-	-	-	-
S89250-100mg买3赠1	≥98%	￥3800.00 S89250-100mg ￥3800.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162)

靶点：

CDK12:6 nM (IC50); Cereblon;CDK; LigandforE3Ligase

体外研究：

BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F. BSJ-4-116 (50 nM; 6-24 hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line. BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein. Cell Proliferation Assay Cell Line: Parental Kelly and CDK12C1039F cells Concentration: 10-10000 nM Incubation Time: 72 hours Result: Antiproliferative activity of BSJ-4-116 is independent of the mutational status, and the degrader compounds exhibited improved GR50 (growth rate inhibition) values in Kelly CDK12C1039F cells compared with the parental cell line. Western Blot Analysis Cell Line: Parental and CDK12C1039F (KellyCDK12CF)-expressing Kelly cells Concentration: 50 nM Incubation Time: 6-24 hours Result: Led to the same level of CDK12 protein level decrease, regardless of the mutational status of the cell line.

细胞实验：

For poly(A) 3'-end sequencing, Jurkat cells are exposed to DMSO or THZ531 (250 nM) or to BSJ-4-116 or BSJ-4-116-NC (50 nM) for 8 h. RNA extraction is performed with TRIzol following the manufacturer's instructions. Total RNA is treated with DNase I. Sequencing libraries are prepared with the RNA-sequencing library kit following the manufacturer's instructions. All samples are sequenced on a HiSeq 2500 sequencer.

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.194 ml	5.971 ml	11.942 ml
5 mM	0.239 ml	1.194 ml	2.388 ml
10 mM	0.119 ml	0.597 ml	1.194 ml
50 mM	0.024 ml	0.119 ml	0.239 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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