product name EHop-016
Description: EHop-016 is a novel potent and selective Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, it is equally potent inhibition for Rac3. Ehop-016 inhibited Rac activity in metastatic cancer cell MDA-MB-435 which overexpressed Rac and inhibited high endogenous Rac activity as well. It also attenuated the effects of Rac downstream protein p21-activated kinase 1 and directed migration of metastatic cancer cells.
References: J Biol Chem. 2012 Apr 13;287(16):13228-38; J Clin Invest. 2013 Oct;123(10):4449-63.
430.55
Formula
C25H30N6O
CAS No.
1380432-32-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Rac inhibition by EHop-016 increases the activity of the closely related Rho GTPase RhoA by a compensatory mechanism. In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits association of active Vav2 with Rac1(G15A) mutant fusion protein, and reduces Rac-regulated cell functions including lamellipodia formation and cell migration. In addition, EHop-016 inhibits cell viability of MDA-MB-435 cells with IC50 of 10 μM. EHop-016 also inhibits KITD814V-induced growth in SM and AML patients-derived cells. Kinase Assay: 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. Cell Assay: 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 manufacturers instructions. |
|---|---|
| In Vivo | Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. |
| Animal model | KITD814V-bearing mice |
| Formulation & Dosage | Dissolved in DMSO; 2.5 μM; i.v. injection. |
| References | J Biol Chem. 2012 Apr 13;287(16):13228-38; J Clin Invest. 2013 Oct;123(10):4449-63. |
