Aminopurvalanol A

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Cyclins/Cdk[1]

Aminopurvalanol A (5 and 40 μM; 8 hours) inhibits cell growth primarily by arresting the cells in the G2 phase of the cell cycle and, at higher concentration, triggering apoptosis[2]. Cell Cycle Analysis[2] Cell Line: Human U937 leukemic cells Concentration: 5 and 40 μM Incubation Time: 8 hours Result: Increased the number of cells with a 4N DNA content as early as 8 h after the beginning of treatment at 5 μM. 40 μM led to cellular fragmentation and cells with an irregular DNA distribution, characteristic of apoptotic cell populations. Apoptosis Analysis[2] Cell Line: Human U937 leukemic cells Concentration: 5 and 40 μM Incubation Time: 8 hours Result: 40 μM Aminopurvalanol A led to apoptosis rather than after the beginning of treatment at 5 μM.

[1]. Bernabò N, et al. Aminopurvalanol A, a Potent, Selective, and Cell Permeable Inhibitor of Cyclins/Cdk Complexes, Causes the Reduction of in Vitro Fertilizing Ability of Boar Spermatozoa, by Negatively Affecting the Capacitation-Dependent Actin Polymerization. Front Physiol. 2017;8:1097.

[2]. Rosania GR, et al. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999;96(9):4797-4802.