EHT 1864
EHT 1864 is a small-molecule inhibitor of Rac family small GTPases with Kd value of 40nM for Rac1 [1].
In NIH 3T3 mouse fibroblasts, EHT 1864 treatment shows an 80% reduction in PDGF-induced lamellipodia formation. EHT 1864 at concentration of 50μM can completely inhibit the complex formation between Rac1 and PAK-RBD and cause the release of nucleotide from Rac1. The reassociation of nucleotide with Rac1 induced by EDTA or the Tiam1 can also be blocked by EHT 1864. EHT 1864 is most potent to Rac1, both in the binding affinity and stimulation of nucleotide release. It binds to Rac1b, Rac2 and Rac3 with Kd values of 50nM, 60nM and 250nM, respectively. Moreover, EHT 1864 can suppress cellular transformation induced by Rac1 with an 80% inhibition of focus-forming activity [1].
References:
[1] Shutes A, Onesto C, Picard V, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Journal of Biological Chemistry, 2007, 282(49): 35666-35678.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 581.48 |
| Cas No. | 754240-09-0 |
| Formula | C25H29Cl2F3N2O4S |
| Solubility | ≥29.05 mg/mL in DMSO with gentle warming; ≥16.53 mg/mL in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(C1=CC=C2C(SCCCCCOC3=COC(CN4CCOCC4)=CC3=O)=CC=NC2=C1)F.Cl.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
INS-1 832/13 cells (Insulin-Producing-Cell Line) |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
1 h |
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Applications |
10 μM EHT 1864 shows a complete inhibition of GSIS (Glucose-stimulated insulin secretion)and inhibits GSIS at 10-20mM glucose. It also suppresses a glucose-induced membrane association of Rac1 and glucose-induced ERK1/2 phosphorylation and activation. |
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References: 1. Sidarala V, Veluthakal R, Syeda K, Kowluru A. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells. Cell Signal. 2015 Jun;27(6):1159-67. | |
| Description | EHT 1864 is a potent inhibitor of Rac family GTPase with Kd values of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. | |||||
| Targets | Rac1 | Rac1b | Rac2 | Rac3 | ||
| IC50 | (Kd=40 nM) | (Kd=50 nM) | (Kd=60 nM) | (Kd=250 nM) | ||
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