Product Name :
EHT 1864
Description:
EHT 1864 is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 attenuates glucose-stimulated insulin secretion in pancreatic β-cells. EHT 1864 specifically inhibits glucose-induced Rac1 activation and membrane association and associated downstream signaling events culminating in inhibition of GSIS.
CAS:
754240-09-0
Molecular Weight:
581.47
Formula:
C25H29Cl2F3N2O4S
Chemical Name:
2-(morpholinomethyl)-5-((5-((7-(trifluoromethyl)quinolin-4-yl)thio)pentyl)oxy)-4H-pyran-4-one dihydrochloride
Smiles :
Cl.Cl.O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC1=CC=NC2=CC(=CC=C12)C(F)(F)F
InChiKey:
LSECOAJFCKFQJG-UHFFFAOYSA-N
InChi :
InChI=1S/C25H27F3N2O4S.2ClH/c26-25(27,28)18-4-5-20-21(14-18)29-7-6-24(20)35-13-3-1-2-10-33-23-17-34-19(15-22(23)31)16-30-8-11-32-12-9-30;;/h4-7,14-15,17H,1-3,8-13,16H2;2*1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Glibornuride} web|{Glibornuride} Inhibitor|{Glibornuride} NF-κB|{Glibornuride} Protocol|{Glibornuride} Purity|{Glibornuride} supplier}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
EHT 1864 is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 attenuates glucose-stimulated insulin secretion in pancreatic β-cells. EHT 1864 specifically inhibits glucose-induced Rac1 activation and membrane association and associated downstream signaling events culminating in inhibition of GSIS.|Product information|CAS Number: 754240-09-0|Molecular Weight: 581.47|Formula: C25H29Cl2F3N2O4S|Synonym:|EHT 1864 HCl|EHT-1864 dihydrochloride|EHT-1864|EHT1864|Chemical Name: 2-(morpholinomethyl)-5-((5-((7-(trifluoromethyl)quinolin-4-yl)thio)pentyl)oxy)-4H-pyran-4-one dihydrochloride|Smiles: Cl.Cl.O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC1=CC=NC2=CC(=CC=C12)C(F)(F)F|InChiKey: LSECOAJFCKFQJG-UHFFFAOYSA-N|InChi: InChI=1S/C25H27F3N2O4S.2ClH/c26-25(27,28)18-4-5-20-21(14-18)29-7-6-24(20)35-13-3-1-2-10-33-23-17-34-19(15-22(23)31)16-30-8-11-32-12-9-30;;/h4-7,14-15,17H,1-3,8-13,16H2;2*1H|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{GLP-1(7-36), amide} medchemexpress|{GLP-1(7-36), amide} GCGR|{GLP-1(7-36), amide} Activator|{GLP-1(7-36), amide} Purity & Documentation|{GLP-1(7-36), amide} In Vitro|{GLP-1(7-36), amide} manufacturer} |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|EHT 1864 selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1.PMID:24187611 EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH 3T3 cells stably expressing H-Ras(61L) protein. EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down.|In Vivo:|EHT 1864 (oral administration) displays good tolerability, brain penetrance, and no genotoxicity. EHT 1864 (10 and 40 mg/kg/day; daily; 15 days; intraperitoneal injections) lowers brain Aβ 40 by 37% in guinea pigs.|References:|Desire L, et al. RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo. J Biol Chem. 2005 Nov 11;280(45):37516-25.Shutes A, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. J Biol Chem. 2007 Dec 7;282(49):35666-78.Onesto C, et al. Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 2008;439:111-29.Products are for research use only. Not for human use.|
