KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest[1][2].
IC 50
p300
References
[1] Shi Q, et al. Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor. ACS Med Chem Lett. 2012 Jun 21;3(8):620-5. DOI:10.1021/ml300042k [2] Wang W, et al. KCN1, a novel synthetic sulfonamide anticancer agent: in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. PLoS One. 2012;7(9):e44883. DOI:10.1371/journal.pone.0044883