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Chemical Structure : BSJ-4-116
CAS No.: 2519823-34-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $188 | In stock | |
| 25 mg | $358 | In stock | |
| 50 mg | $598 | In stock | |
| 100 mg | $958 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 837.39 | |
| Formula | C40H49ClN8O8S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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]- |
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1. Baishan Jiang, et al. Nat Chem Biol. 2021 Jun;17(6):675-683.
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