Date published: 2025-10-2

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EHT 1864 (CAS 754240-09-0)

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Alternate Names:
EHT 1864 is known as a Rac inhibitor, part of a subfamily of Rho GTPases.
Application:
EHT 1864 is an antiproliferative inhibitor of Rac family GTPases, directly binding to Rac1, Rac1b, Rac2, and Rac3.
CAS Number:
754240-09-0
Purity:
≥97%
Molecular Weight:
581.47
Molecular Formula:
C25H27F3N2O4S•2HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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EHT 1864 is a highly potent and selective Rac1 inhibitor, showcasing a remarkable affinity for the Rac family of GTPases, which are pivotal in the regulation of cell shape, migration, and growth through their control of actin cytoskeleton dynamics. Its mechanism of action is predicated on the stabilization of Rac in its inactive GDP-bound state, effectively preventing its interaction with downstream effectors that are critical for actin filament organization. This unique inhibitory capability makes EHT 1864 an invaluable tool in cellular biology and molecular research, as it allows for the precise dissection of Rac1-mediated signaling pathways. Researchers leverage EHT 1864 to unravel the complex roles of Rac1 in various cellular processes, including cell motility, adhesion, and proliferation, providing insights into the fundamental mechanisms that underpin cellular behavior and response to external stimuli. Its specificity and potency are instrumental in studying the nuanced roles of Rac1, facilitating advancements in our understanding of cytoskeletal organization and its implications for cell physiology.


EHT 1864 (CAS 754240-09-0) References

  1. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.  |  Shutes, A., et al. 2007. J Biol Chem. 282: 35666-78. PMID: 17932039
  2. Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.  |  Onesto, C., et al. 2008. Methods Enzymol. 439: 111-29. PMID: 18374160
  3. Inhibition of the Rho GTPase, Rac1, decreases estrogen receptor levels and is a novel therapeutic strategy in breast cancer.  |  Rosenblatt, AE., et al. 2011. Endocr Relat Cancer. 18: 207-19. PMID: 21118977
  4. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells.  |  Sidarala, V., et al. 2015. Cell Signal. 27: 1159-67. PMID: 25725286
  5. The effect of Rho drugs on mast cell activation and degranulation.  |  Sheshachalam, A., et al. 2017. J Leukoc Biol. 102: 71-81. PMID: 28411215
  6. Inhibition of Rac family protein impairs colitis and colitis-associated cancer in mice.  |  Guo, Y., et al. 2018. Am J Cancer Res. 8: 70-80. PMID: 29416921
  7. Rac-GTPase promotes fibrotic TGF-β1 signaling and chronic kidney disease via EGFR, p53, and Hippo/YAP/TAZ pathways.  |  Patel, S., et al. 2019. FASEB J. 33: 9797-9810. PMID: 31095421
  8. Rac1 Promotes Cell Motility by Controlling Cell Mechanics in Human Glioblastoma.  |  Xu, J., et al. 2020. Cancers (Basel). 12: PMID: 32585958
  9. Immunogenomic Profiling and Classification of Prostate Cancer Based on HIF-1 Signaling Pathway.  |  Song, J., et al. 2020. Front Oncol. 10: 1374. PMID: 32850440
  10. S1PR2 Inhibition Attenuates Allergic Asthma Possibly by Regulating Autophagy.  |  Liu, H., et al. 2020. Front Pharmacol. 11: 598007. PMID: 33643037
  11. Molecular Mechanisms of the Blockage of Glioblastoma Motility.  |  Xu, J., et al. 2021. J Chem Inf Model. 61: 2967-2980. PMID: 33861592
  12. RAC1 plays an essential role in estrogen receptor alpha function in breast cancer cells.  |  Sun, J., et al. 2021. Oncogene. 40: 5950-5962. PMID: 34373577
  13. Rac GTPases in acute myeloid leukemia cells: Expression profile and biological effects of pharmacological inhibition.  |  Ramos, DFV., et al. 2022. Toxicol Appl Pharmacol. 442: 115990. PMID: 35331739
  14. Hyperglycemic Conditions Promote Rac1-Mediated Serine536 Phosphorylation of p65 Subunit of NFκB (RelA) in Pancreatic Beta Cells.  |  Kowluru, A., et al. 2022. Cell Physiol Biochem. 56: 367-381. PMID: 35981264
  15. Identifying the molecular mechanisms of sepsis-associated acute kidney injury and predicting potential drugs.  |  Guo, G., et al. 2022. Front Genet. 13: 1062293. PMID: 36579331

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

EHT 1864, 10 mg

sc-361175
10 mg
$209.00

EHT 1864, 50 mg

sc-361175A
50 mg
$872.00