AIM100 是选择性的 ACK1 抑制剂 (IC50:21.58 nM)。它还抑制 Tyr267磷酸化,但不抑制其他激酶,包括 PI3K 和 Akt 亚家族成员。它具有抗癌活性。
产品描述
AIM-100 is a Ack1 inhibitor (IC50: 24 nM).
体外活性
AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase [1]. It 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].
Cas No.
873305-35-2
分子式
C23H21N3O2
分子量
371.44
别名
AIM100
储存和溶解度
Ethanol:30 mg/mL
DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years