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| CAS: | 2519823-34-6 | Cat No: | JKN03302 | Purity: | 98% |
Note: All products of the company are for scientific research only, and do not provide products and services for any individual
Product Description
| CAS | 2519823-34-6 | Cat No | JKN03302 | |
| Name | BSJ-4-116 | |||
| Synonyms | BSJ-4-116 | |||
| Smiles | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)N[C@@H]3CCCN(C3)CCCCCCCNC(=O)COC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O | |||
| Chemical Name | N-[7-[(3R)-3-[[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]piperidin-1-yl]heptyl]-2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetamide | |||
| Formula | C40H49ClN8O8S | MWt | 837.4 | |
| Purity | 98% | Storage | Store at 4--8℃ | |
| Description | BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 selectively degraded CDK12 as assessed through quantitative proteomics. Selective degradation of CDK12 resulted in premature cleavage and poly(adenylation) of DDR genes. Moreover, BSJ-4-116 exhibited potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor olaparib, as well as when used as a single agent against cell lines resistant to covalent CDK12 inhibitors. Two point mutations in CDK12 were identified that confer resistance to BSJ-4-116, demonstrating a potential mechanism that tumor cells can use to evade bivalent degrader. | |||
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