BSJ-4-116 |CAS:2519823-34-6 Probechem Biochemicals

Chemical Structure : BSJ-4-116

CAS No.: 2519823-34-6

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BSJ-4-116 (CDK12 PROTAC BSJ-4-116)

货号: PC-38058Not For Human Use, Lab Use Only.

BSJ-4-116 is a potent, CDK12 specific degrader (PROTAC) with IC50 of 6 nM, exhibits anti-proliferative activity in cancer cells.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3580	In stock
50 mg	￥5480	In stock
100 mg		Get quote

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生物&药学活性

BSJ-4-116 is a potent, CDK12 specific degrader (PROTAC) with IC50 of 6 nM, exhibits anti-proliferative activity in cancer cells.
BSJ-4-116 demonstrates a low nanomolar IC50 for inhibiting CDK12 enzymatic activity and exhibits potent CDK12 degradation in Jurkat cells in a dose- and time-dependent manner, while CDK13 protein level was minimally affected.
BSJ-4-116 also significantly suppresses the phosphorylation of Pol II Ser2 and Thr4, whereas p-Ser5 and p-Ser7 are not inhibited, and not affect the Cyclin K protein level.
BSJ-4-116 downregulates the expression of DDR genes and exhibits anti-proliferative activity in cancer cells.
BSJ-4-116 alone or in combination with PARP inhibitors could be a therapeutic avenue for targeting the intrinsic genomic instability inT-ALL model.
BSJ-4-116 overcomes resistance towards existing covalent inhibitors.

物理化学性质&存储条件

分子量	837.39
分子式	C40H49ClN8O8S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-

参考文献

1. Baishan Jiang, et al. Nat Chem Biol. 2021 Jun;17(6):675-683.

BSJ-4-116 (CDK12 PROTAC BSJ-4-116)

生物&药学活性

物理化学性质&存储条件

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BSJ-4-116 (CDK12 PROTAC BSJ-4-116)

生物&药学活性

物理化学性质&存储条件

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