BSJ-4-116 |
| カタログ番号GC62263 |
BSJ-4-116 は、Cereblon と CDK のリガンドで接続された PROTAC です。 BSJ-4-116 は、IC50 が 6 nM の非常に強力で選択的な CDK12 分解剤 (PROTAC) です。 BSJ-4-116 は、主にポリ (アデニル化) の増加を通じて、転写の早期終結を通じて DDR 遺伝子をダウンレギュレートします。 BSJ-4-116 は、単独で、またはポリ (ADP-リボース) ポリメラーゼ阻害剤オラパリブと組み合わせて、強力な抗増殖効果を示します。
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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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