Product Details of 13325-10-5In 2022 ,《Discovery of Small-Molecule Degraders of the CDK9-Cyclin T1 Complex for Targeting Transcriptional Addiction in Prostate Cancer》 was published in Journal of Medicinal Chemistry. The article was written by Li, Jiacheng; Liu, Ting; Song, Yuanli; Wang, Mingyu; Liu, Liping; Zhu, Hongwen; Li, Qi; Lin, Jin; Jiang, Hualiang; Chen, Kaixian; Zhao, Kehao; Wang, Mingliang; Zhou, Hu; Lin, Hua; Luo, Cheng. The article contains the following contents:
Aberrant hyperactivation of cyclins results in carcinogenesis and therapy resistance in cancers. Direct degradation of the specific cyclin or cyclin-dependent kinase (CDK)-cyclin complex by small-mol. degraders remains a great challenge. Here, we applied the first application of hydrophobic tagging to induce degradation of CDK9-cyclin T1 heterodimer, which is required to keep productive transcription of oncogenes in cancers. LL-K9-3 (I) was identified as a potent small-mol. degrader of CDK9-cyclin T1. Quant. and time-resolved proteome profiling exhibited LL-K9-3-induced selective and synchronous degradation of CDK9 and cyclin T1. The expressions of androgen receptor (AR) and cMyc were reduced by LL-K9-3 (I) in 22RV1 cells. LL-K9-3 (I) exhibited enhanced anti-proliferative and pro-apoptotic effects compared with its parental CDK9 inhibitor SNS032 and suppressed downstream signaling of CDK9 and AR more effectively than SNS032. Moreover, LL-K9-3 (I) inhibited AR and Myc-driven oncogenic transcriptional programs and exerted stronger inhibitory effects on several intrinsic target genes of AR than the monomeric CDK9 PROTAC (Thal-SNS032). After reading the article, we found that the author used 4-Aminobutan-1-ol(cas: 13325-10-5Product Details of 13325-10-5)
4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Product Details of 13325-10-5
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