Drug intelligence / Profile preview

alsterpaullone

Development stage
Unknown
Modality
Small Molecules
01

Overview

Alsterpaullone is a synthetic small molecule belonging to the benzazepine class. It acts as a potent and reversible inhibitor of several cyclin-dependent kinases (CDKs), including CDK1/cyclin B, CDK2/cyclin A/E, and CDK5/p25/p35 complexes. Additionally, it inhibits glycogen synthase kinase 3 beta (GSK‑3β). Alsterpaullone competes with ATP for binding to these kinases and blocks cell cycle progression at G2/M phase. It induces apoptosis in cancer cells by activating caspase pathways—specifically caspase‑8 and caspase‑9—often via mitochondrial membrane potential disruption. The compound has demonstrated antitumor activity in vitro but is not approved for clinical use; its primary application remains in research settings focused on cell cycle regulation and apoptosis mechanisms[1][2][4][5][6][7].

Other names
9-Nitropaullone9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one9-nitro-7,12-dihydroindolo(3,2-d)(1)benzazepin-6(5H)-one
02

Targets

GSK3 (Glycogen synthase kinase 3 beta)CDK1 (Cyclin-dependent kinase 1)CDK2 (Cyclin-dependent kinase 2)CDK5 (Cyclin-dependent kinase 5)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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