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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].

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