"目录号: HY-15290
Protein Tyrosine Kinase/RTK-
AIM-100是Ack1抑制剂，IC50为24 nM。
Ack1
相关产品
KRCA-0008-
生物活性
Description
AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.IC50 value: 24 nM [3]Target: Ack1Ack1 inhibitor AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase [1].The Ack1 inhibitor AIM-100 not only inhibited Ack1 activity but also was able to suppress AR Tyr(267) phosphorylation and its recruitment to the ATM enhancer. Notably, AIM-100 suppressed Ack1 mediated ATM expression and mitigated the growth of radioresistant CRPC tumors [2]. AIM-100, not only inhibited Ack1 activation but also able to suppress pTyr267-AR phosphorylation, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity [3].
References
[1].Mahajan K, et al. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Am J Pathol. 2012 Apr;180(4):1386-93.
[2].Mahajan K, et al. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. J Biol Chem. 2012 Jun 22;287(26):22112-22.
[3].Mahajan K, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010 Sep 1;70(12):1274-85.