Compound class:
Synthetic organic
Comment: LL-K9-3 is a small-molecule that induces simultaneous degradation of CDK9 and cyclin T1 (CDK9-Cyclin T1 heterodimers) that was developed for anti-tumour potential in transcriptionally addicted cancers [1]. It uses hydrophobic tagging technology (HyT) to induce polyubiquitination of CDK9-cyclin T1 complexes, as a mechanism to promote proteasome-mediated degradation of both proteins. In particular LL-K9-3 was evaluated for its inhibitory effects on CDK9 and androgen receptor-mediated signalling pathways in prostate cancer. LL-K9-3 elicits more potent anti-proliferative and pro-apoptotic effects than its parental CDK9 inhibitor BMS-387032 (a.k.a. SNS032), or than the CDK9-only PROTAC THAL-SNS-032.
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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-((2-(2-(((1R, 2S, 5R)-2-isopropyl-5-methylcyclohexyl)oxy) acetamido)ethyl)sulfonyl)piperidine-4-carboxamide |
Database Links | |
GtoPdb PubChem SID | 472319229 |
PubChem CID | 164946948 |
Search Google for chemical match using the InChIKey | NPRIWHDFWDSJRZ-YFNKSVMNSA-N |
Search Google for chemicals with the same backbone | NPRIWHDFWDSJRZ |
UniChem Compound Search for chemical match using the InChIKey | NPRIWHDFWDSJRZ-YFNKSVMNSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | NPRIWHDFWDSJRZ-YFNKSVMNSA-N |