EHT 1864
EHT 1864 (CAS: 754240-09-0) is a small-molecule inhibitor targeting Rac family GTPases, with strongest affinity and inhibitory activity toward Rac1. It interacts directly with Rac isoforms Rac1, Rac1b, Rac2, and Rac3, exhibiting Kd values of approximately 40 nM, 50 nM, 60 nM, and 250 nM, respectively. By disrupting nucleotide binding, EHT 1864 blocks Rac1 activation and prevents the formation of active Rac1/PAK-RBD complexes, thus inhibiting downstream cellular functions, such as PDGF-stimulated lamellipodia formation and Rac1-mediated cellular transformation. This compound serves as a valuable tool in cell biology research for studying Rac-dependent signaling pathways and cellular dynamics.
| 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]: | |
|
Cell lines |
INS-1 832/13 cells (Insulin-Producing-Cell Line) |
|
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. |
|
Reaction Conditions |
1 h |
|
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. |
|
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) | ||
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
