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EHT 1864

CAT: 0804-HY-16659-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16659-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG[1][2][3][4].
CAS Number
754240-09-0
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Ras
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Neurological Disease; Cancer
Assay Protocol
https://www.medchemexpress.com/EHT-1864.html
Purity
99.85
Solubility
DMSO : ≥ 32 mg/mL|H2O : ≥ 100 mg/mL
Smiles
O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34.[H]Cl.[H]Cl
Molecular Formula
C25H29Cl2F3N2O4S
Molecular Weight
581.48
Precautions
H302, H315, H319, H335
References & Citations
[1]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.|[2]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.|[3]Onesto C, et al. Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 2008;439:111-29.|[4]Ying Liu , et al. Podocyte-Released Migrasomes in Urine Serve as an Indicator for Early Podocyte Injury. Kidney Dis (Basel) . 2020 Nov;6 (6) :422-433.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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