EHop016 是一种特异性 Rac GTPase 抑制剂，对 MDA-MB-231 和 MDA-MB-435 细胞中的 Rac1 的 IC50 为 1.1 μM，也可抑制Rac3 。它还抑制 Vav2 与 Rac，Rac 激活的 PAK1 相互作用，片状脂蛋白形成和细胞迁移。

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.

EHop-016使患有KITD814V细胞的白血病小鼠存活率得到显著提高.

在MDA-MB-435细胞中,EHop-016（2-5 μM）抑制活性VAV2与Rac1（G15A）突变体融合蛋白的结合,并使Rac调控的细胞功能减少,包括板状伪足形成和细胞迁移。由于代偿机制,EHop-016对Rac的抑制增加了与之密切相关的Rho GTPase RhoA活性。此外,EHop-016抑制MDA-MB-435细胞的细胞活性（IC50：10 μM）。 EHop-016还抑制了来自SM和AML患者的细胞中KITD814V诱导的生长。

Rac Activity Assays: Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines (from ATCC). Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit.

MDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells (from ATCC) are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.(Only for Reference)

1380432-32-5

C25H30N6O

430.556

EHop 016

DMSO:21.5 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years