COA | MSDS | HPLC | NMR |
CAS No: | 1380432-32-5 |
Molecular formula(MF) | C25H30N6O |
Molecular Weight(MW): | 430.55 |
Alias |
In vitro | DMSO | 86 mg/mL (199.74 mM) |
---|---|---|
Water | <1 mg/mL | |
Ethanol | <1 mg/mL | |
In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 5mg/mL |
Description | EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3. | ||
---|---|---|---|
Targets |
|
||
In vitro |
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. [1] EHop-016 also inhibits KITD814V-induced growth in SM and AML patients-derived cells. [2] |
||
In vivo | Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. [2] |