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BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $50 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $396 | In Stock | |
50 mg | $637 | In Stock | |
100 mg | $953 | In Stock | |
1 mL x 10 mM (in DMSO) | $173 | In Stock |
Description | BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). |
Targets&IC50 | CDK12:6 nM |
In vitro | 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 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.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. |
Molecular Weight | 837.38 |
Formula | C40H49ClN8O8S |
Cas No. | 2519823-34-6 |
Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCC(NCCCCCCCN4C[C@H](NC=5N=C(NC6=C(S(C(C)C)(=O)=O)C=CC=C6)C(Cl)=CN5)CCC4)=O |
Relative Density. | 1.368 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (298.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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