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EHop-016

(CAS No:1380432-32-5)
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.
CAS No:1380432-32-5
Molecular Weight(MW):430.55
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1380432-32-5
Molecular formula(MF) C25H30N6O
Molecular Weight(MW): 430.55
Alias
Solubility
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
Biological Activity
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
Rac1 [1]
(MDA-MB-435, MDA-MB-231 cells)
1.1 μM
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]