Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Nature Chemical Biology called Discovery and resistance mechanism of a selective CDK12 degrader, Author is Jiang, Baishan; Gao, Yang; Che, Jianwei; Lu, Wenchao; Kaltheuner, Ines H.; Dries, Ruben; Kalocsay, Marian; Berberich, Matthew J.; Jiang, Jie; You, Inchul; Kwiatkowski, Nicholas; Riching, Kristin M.; Daniels, Danette L.; Sorger, Peter K.; Geyer, Matthias; Zhang, Tinghu; Gray, Nathanael S., which mentions a compound: 882562-40-5, SMILESS is ClC1=NC(C2=CN(C3=C2C=CC=C3)S(=O)(=O)C2=CC=CC=C2)=C(Cl)C=N1, Molecular C18H11Cl2N3O2S, Name: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole.
Cyclin-dependent kinase 12 (CDK12) is an emerging therapeutic target due to its role in regulating transcription of DNA-damage response (DDR) genes. However, development of selective small mols. targeting CDK12 has been challenging due to the high degree of homol. between kinase domains of CDK12 and other transcriptional CDKs, most notably CDK13. In the present study, the rational design and characterization of a CDK12-specific degrader, BSJ-4-116 (I), is reported. BSJ-4-116 selectively degraded CDK12 as assessed through quant. 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 mols.
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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem