EHop-016

• CAT Number: I001468
• CAS Number: 1380432-32-5
• Molecular Formula: C25H30N6O
• Molecular Weight: 430.556
• Purity: ≥95%
• Target: Rho
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: Store at -20 C
• IC50: 1.1 uM (MDA-MB-435 cell) [1]
• IUPAC Name: 4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine
• InChI: InChI=1S/C25H30N6O/c1-2-31-22-7-4-3-6-20(22)21-18-19(8-9-23(21)31)28-24-10-12-27-25(29-24)26-11-5-13-30-14-16-32-17-15-30/h3-4,6-10,12,18H,2,5,11,13-17H2,1H3,(H2,26,27,28,29)
• InChIKey: AFTZZRFCMOAFCR-UHFFFAOYSA-N
• SMILES: CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51

EHop-016(CAT: I001468) is a small molecule inhibitor of Rac GTPases, which are important regulators of cytoskeletal dynamics, cell migration, and invasion. Rac GTPases play a key role in cancer cell invasion and metastasis, and their activity is often dysregulated in various types of cancer. EHop-016 works by selectively inhibiting the activity of Rac GTPases, which can prevent cancer cell migration and invasion, and enhance the sensitivity of cancer cells to chemotherapy and radiation therapy. EHop-016 has shown promising results in preclinical studies, particularly in the treatment of breast cancer and melanoma. It has been found to be effective in inhibiting tumor growth and metastasis, as well as reversing drug resistance.

Reference

1:Pharmacokinetics of Rac inhibitor EHop-016 in mice by ultra-performance liquid chromatography tandem mass spectrometry. Humphries-Bickley T, Castillo-Pichardo L, Corujo-Carro F, Duconge J, Hernandez-O/’Farrill E, Vlaar C, Rodriguez-Orengo JF, Cubano L, Dharmawardhane S.J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Feb 15;981-982:19-26. doi: 10.1016/j.jchromb.2014.12.021. Epub 2015 Jan 2. PMID: 25594952 Free PMC Article2:The Rac Inhibitor EHop-016 Inhibits Mammary Tumor Growth and Metastasis in a Nude Mouse Model. Castillo-Pichardo L, Humphries-Bickley T, De La Parra C, Forestier-Roman I, Martinez-Ferrer M, Hernandez E, Vlaar C, Ferrer-Acosta Y, Washington AV, Cubano LA, Rodriguez-Orengo J, Dharmawardhane S.Transl Oncol. 2014 Oct 24;7(5):546-55. doi: 10.1016/j.tranon.2014.07.004. eCollection 2014 Oct. PMID: 25389450 Free PMC Article3:Development of EHop-016: a small molecule inhibitor of Rac. Dharmawardhane S, Hernandez E, Vlaar C.Enzymes. 2013;33 Pt A:117-46. doi: 10.1016/B978-0-12-416749-0.00006-3. Epub 2013 Aug 8. Review. PMID: 25033803 4:Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. Montalvo-Ortiz BL, Castillo-Pichardo L, Hernández E, Humphries-Bickley T, De la Mota-Peynado A, Cubano LA, Vlaar CP, Dharmawardhane S.J Biol Chem. 2012 Apr 13;287(16):13228-38. doi: 10.1074/jbc.M111.334524. Epub 2012 Mar 1. PMID: 22383527 Free PMC Article