Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
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1 mg | 在庫あり | ¥ 14,500 | |||
5 mg | 在庫あり | ¥ 30,500 | |||
10 mg | 在庫あり | ¥ 52,000 | |||
25 mg | 在庫あり | ¥ 112,500 | |||
50 mg | 在庫あり | ¥ 166,000 | |||
100 mg | 在庫あり | ¥ 226,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 45,500 |
説明 | 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). |
ターゲット&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. |
分子量 | 837.38 |
分子式 | C40H49ClN8O8S |
CAS No. | 2519823-34-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (298.55 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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BSJ-4-116 2519823-34-6 Cell Cycle/Checkpoint PROTAC Ligand for E3 Ligase CDK degrader antiproliferative inhibit Kelly C1039F BSJ 4 116 Cyclin dependent kinase PROTACs cancer Inhibitor CDK12 mutation BSJ4116 inhibitor