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N-methyl-{4-[2-(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)hydrazino]phenyl}methanesulfonamide

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
01

Overview

N-methyl-{4-[2-(7‑oxo‑6,7‑dihydro‑8H‑[1,3]thiazolo[5,4-e]indol‑8‑ylidene)hydrazino]phenyl}methanesulfonamide is a synthetic small molecule belonging to the class of oxindole-based compounds. It was developed as a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2), an enzyme involved in cell cycle regulation. Structural studies have shown this compound binds to CDK2 with high affinity and selectivity over related kinases such as CDK1. In preclinical research settings it has demonstrated low nanomolar inhibitory activity against CDK2 and can induce cell cycle arrest. This compound has been studied primarily for its potential utility in modulating cell proliferation and for possible prevention of chemotherapy-induced alopecia; however there are no approved clinical indications or ongoing clinical trials for this agent at present.[1][2][6]

Other names
N-Methyl-(4-(2-(7-oxo-6,7-dihydro-8H-(1,3)thiazolo(5,4-e)indol-8-ylidene)hydrazino)phenyl)methanesulfonamideN-methyl-{4-[2-(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-yilidene)hydrazino]phenyl}methanesulfonamideN-methyl-{4-[2-(7-OXO–6,7-DIHYDRO–8H–[1,3]-THIAZOLO[5,4-E]-INDOL–8-YLIDENE)-HYDRAZINO]-PHENYL}-METHANESULFONAMIDE
02

Targets

CDK2 (Cyclin-dependent kinase 2)

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