AIM-100

AIM-100 is a potent and selective small molecule inhibitor of activated Cdc42 kinase 1 (Ack1), also known as tyrosine non-receptor kinase 2 (TNK2). It inhibits Ack1/TNK2 with an IC50 of approximately 21.58–24 nM and shows high selectivity over other kinases. Mechanistically, AIM-100 mimics ATP to inhibit Ack1 activity and does not significantly inhibit a panel of other kinases including PI3K and AKT. In cellular models such as human prostate cancer cells (LNCaP, LAPC4) and pancreatic cancer cells (Panc‑1), it induces cell cycle arrest in G0/G1 phase and suppresses cell growth; it also induces apoptosis at higher concentrations. Additionally, AIM‑100 inhibits androgen receptor transcriptional activity by suppressing phosphorylation events downstream of Ack1 activation. Its primary use is in research settings for studying the role of Ack1/TNK2 in cancer biology[1][3][4][5].

Other names

N-{[(2S)-oxolan-2-yl]methyl}-5,6-diphenylfuro[2,3-d]pyrimidin-4-amine