EHop-016 (CAS 1380432-32-5)
Alternate Names:
N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine
CAS Number:
1380432-32-5
Molecular Weight:
430.55
Molecular Formula:
C25H30N6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
EHop-016 is a potent inhibitor of Rac GTPase, specifically targeting Rac1 with an IC50 of 1.1 μM in MDA-MB-435 and MDA-MB-231 cells. It also exhibits equally robust inhibition of Rac3. Interestingly, the inhibition of Rac by EHop-016 triggers a compensatory mechanism that enhances the activity of the closely related Rho GTPase, RhoA. In MDA-MB-435 cells, EHop-016 (2-5 μM) disrupts the association between active Vav2 and the Rac1(G15A) mutant fusion protein, leading to the suppression of Rac-dependent cellular processes, including lamellipodia formation and cell migration. Furthermore, EHop-016 exhibits significant inhibition of cell viability in MDA-MB-435 cells, with an IC50 value of 10 μM. Notably, it also demonstrates efficacy in inhibiting KITD814V-induced growth in cells derived from SM and AML patients.
EHop-016 (CAS 1380432-32-5) References
- Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. | Montalvo-Ortiz, BL., et al. 2012. J Biol Chem. 287: 13228-38. PMID: 22383527
- Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. | Martin, H., et al. 2013. J Clin Invest. 123: 4449-63. PMID: 24091327
- Development of EHop-016: a small molecule inhibitor of Rac. | Dharmawardhane, S., et al. 2013. Enzymes. 33 Pt A: 117-46. PMID: 25033803
- The Rac Inhibitor EHop-016 Inhibits Mammary Tumor Growth and Metastasis in a Nude Mouse Model. | Castillo-Pichardo, L., et al. 2014. Transl Oncol. 7: 546-55. PMID: 25389450
- Pharmacokinetics of Rac inhibitor EHop-016 in mice by ultra-performance liquid chromatography tandem mass spectrometry. | Humphries-Bickley, T., et al. 2015. J Chromatogr B Analyt Technol Biomed Life Sci. 981-982: 19-26. PMID: 25594952
- VAV2, a guanine nucleotide exchange factor for Rac1, regulates glucose-stimulated insulin secretion in pancreatic beta cells. | Veluthakal, R., et al. 2015. Diabetologia. 58: 2573-81. PMID: 26224100
- Design, synthesis and biological evaluation of new carbazole derivatives as anti-cancer and anti-migratory agents. | Vlaar, CP., et al. 2018. Bioorg Med Chem. 26: 884-890. PMID: 29358027
- Long noncoding RNA LCAT1 functions as a ceRNA to regulate RAC1 function by sponging miR-4715-5p in lung cancer. | Yang, J., et al. 2019. Mol Cancer. 18: 171. PMID: 31779616
- In Vitro Antimalarial Activity of Inhibitors of the Human GTPase Rac1. | Parapini, S., et al. 2022. Antimicrob Agents Chemother. 66: e0149821. PMID: 34723630
- The Mechanism of Rac1 in Regulating HCC Cell Glycolysis Which Provides Underlying Therapeutic Target for HCC Therapy. | Ren, YX., et al. 2022. J Oncol. 2022: 7319641. PMID: 35847360
- 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
- NPM1-Mutated Patient-Derived AML Cells Are More Vulnerable to Rac1 Inhibition. | Hemsing, AL., et al. 2022. Biomedicines. 10: PMID: 36009428
- The Rac inhibitor HV-107 as a potential therapeutic for metastatic breast cancer. | Crespo, GV., et al. 2023. Mol Med. 29: 75. PMID: 37316799
Inhibitor of:
β2-chimaerin, ARHGEF17, ARHGEF9, Atlastin, C11orf2, Cdc42EP3, Centaurin γ3, CHM Rab escort protein, CIP4, D6Wsu116e, DBC-2, DDEF2, DOCK 6, DOCK 7, EG434881, Elmo1, EPI64, Espin, Ezrin, FAM21B, FGD5, GRP1, HIP1, Integrin α6, IQSEC2, ITFG2, KBTBD6, MICAL1, MRCKγ, P-Rex1, PACS-1b, Rab 5B, Rab GDI (GDP dissociation inhibitor), rabphilin-11, Rac 1, Rac 2, Rac 3, Rac GAP1, racrac2, RAPGEF5, RASA4B, REEP5, Rho 8, Rhotekin, Rnd1, Vav, and WRCH1.Activator of:
βPIX, γPAK, ARHGAP10, ARHGAP11A, ARHGAP24, ARHGEF38, BC057079, CED-5, Crk-L, D230039L06Rik, D6Wsu116e, DOCK 180, Drac1/2, FARP1, FMNL2, Gα 13, HEPN1, IL-5, Integrin α8, KLHL38, Lfc, Rab 5A, Ron, and Tiam2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
EHop-016, 5 mg | sc-497382 | 5 mg | $80.00 |