AIM-100 modulates ligand-independent AR activity and inhibits prostate cell growth.
aim-100 is a small inhibitor of ack1 tyrosine kinase with ic50 value of 24 nm [1].aim-100 mimicked atp and inhibited the activity of ack1 significantly and specifically. it showed no inhibition activity for the other 30 kinases including pi3-kinase and akt, and showed a five-fold higher ic50 value for lck. in mef cells treated with egf, aim-100 caused a remarkable decrease of the activation of ack1. in the human prostate cancer cells lncap and lapc4, aim-100 treatment resulted in an increase of g0/g1 cell phase and subsequent cell growth suppression. these effects of aim-100 also exerted in the pancreatic cancer cells. aim-100 induced apoptosis in panc-1 cells at concentration of 10 μm. moreover, aim-100 inhibited cell growth with gi50 values of 7 to 8 μm in cd-18, panc-1, ov90, mcf-7 and mda-mb-468 cancer cells [1, 2].
1. mahajan k, challa s, coppola d, et al. effect of ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. the prostate, 2010, 70(12): 1274-1285. 2. mahajan k, coppola d, chen y, et al. ack1 tyrosine kinase activation correlates with pancreatic cancer progression. the american journal of pathology, 2012, 180(4): 1386-1393.
