EHop-016

EHop-016 is an inhibitor of the small Rho GTPases Rac1 and Rac3. It inhibits Rac1 activity in MDA-MB-435 breast cancer cells with an IC50 value of 1.1 µM in a Rac1 activation assay. At a concentration of 1 µM, EHop-016 inhibits 58% of Rac3 activity, and it inhibits Cdc42 activity but only at higher concentrations (5-10 µM). It also increases Rho GTPase RhoA activity ~1.3-fold at concentrations greater than 2 µM. EHop-016 (2-4 µM) inhibits Rac-regulated functions in MDA-MB-435 cells, including lamellipodia formation and serine/threonine p21-activated kinase 1 (PAK1)-mediated cell migration. In a nude mouse model of breast cancer metastasis, EHop-016 (25 mg/kg) significantly lowers mammary fat pad tumor growth, metastasis, and angiogenesis. It also inhibits mutant receptor tyrosine kinase (KIT)-induced growth in systemic mastocytosis and acute myeloid leukemia (AML) cells (>2.5 µM).Formal Name: N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine. CAS Number: 1380432-32-5. Molecular Formula: C25H30N6O. Formula Weight: 430.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2), (1:7): 0.125, DMSO: 10 mg/ml. lambdamax: 232, 305 nm. SMILES: CCN(C1=C2C=CC=C1)C(C2=C3)=CC=C3NC4=NC(NCCCN5CCOCC5)=NC=C4. InChi Code: 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). InChi Key: AFTZZRFCMOAFCR-UHFFFAOYSA-N.