AIM-100

AIM-100 is a potent and selective Ack1 inhibitor with an IC₅₀ of 21.58 nM. AIM-100 also inhibits Tyr²⁶⁷ phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect^[1][2]. IC50 & Target: IC50: 21.58 nM (Ack1)^[2] In Vitro: AIM-100 (2-10 μM; 48 hours) treatment not only inhibits Ack1 activation but also suppresses AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase. AIM-100 not only inhibits Ack1/AKT Tyr-phosphorylation but also suppressed growth of cell lines derived from pancreatic, breast, and lung tumors^[1].
The Ack1 inhibitor AIM-100 not only inhibited Ack1 activity but also was able to suppress AR Tyr²⁶⁷ phosphorylation and its recruitment to the ataxia-telangiectasia mutated kinase (ATM) enhancer^[2].
AIM-100 is able to suppress pTyr²⁶⁷-AR phosphorylation, binding of androgen receptor (AR) to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity^[3]. In Vivo: In male nude castrated mice, AIM-100 (4 mg/kg) suppresses growth of radioresistant castration-resistant prostate cancer (CRPC) xenograft tumors by decreasing ataxia-telangiectasia mutated kinase (ATM) expression^[2].