EHop-016

Description

Description

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1, equally potent inhibition for Rac3.

1.1 μM ^[1]

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]

Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. ^[2]

EHop-016

Catalog No.S7319

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1, equally potent inhibition for Rac3.

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10mg	USD 122	In stock	0 1 2 3 4 5 6 7 8 9 10
25mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

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.

Cell lines	MDA-MB-231, MDA-MB-435, or MCF-10A cells
Concentrations	~10 μM
Incubation Time	24 hours
Method	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.

Animal Models	KITD814V-bearing mice.
Dosages	2.5 μM
Administration	KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL

Solubility (25°C) *	In vitro	DMSO	86 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.