BSJ-4-116 |
| Catalog No.GC62263 |
BSJ-4-116은 Cereblon 및 CDK용 리간드로 연결된 PROTAC입니다. BSJ-4-116은 IC50이 6nM인 매우 강력하고 선택적인 CDK12 분해제(PROTAC)입니다. BSJ-4-116은 주로 폴리(아데닐화) 증가를 통해 전사의 조기 종결을 통해 DDR 유전자를 하향 조절합니다. BSJ-4-116은 단독으로 그리고 폴리(ADP-리보스) 중합효소 억제제 올라파립과 함께 강력한 항증식 효과를 나타냅니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2519823-34-6
Sample solution is provided at 25 µL, 10mM.
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BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib [1].
BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F[1].BSJ-4-116 (50 nM; 6-24 hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line[1].BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition[1]. 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[1].
[1]. Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683.
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