GNE-2861

GNE-2861 is an inhibitor of the group 2 p21-activated kinases (PAKs, IC50s = 7.5, 126, and 36 nM for PAK4, -5, and -6, respectively). It is selective for group 2 PAKs over group 1 PAKs (IC50s = 5.42, 0.97, and >10 µM for PAK1, -2, and -3, respectively), as well as JAK3, KHS1, MAP4K4, and MINK1 at 1 µM. GNE-2861 (0.1-50 µM) inhibits cell migration and reduces cell viability of MDA-MB-436 and MCF-10A PIK3CA cells in a concentration-dependent manner. It sensitizes drug-resistant MCF-7/LCC2 breast cancer cells to tamoxifen (Cay-13258).Formal Name: 1-[2-[1-(2-amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]-cyclohexanol. CAS Number: 1394121-05-1. Molecular Formula: C22H26N6O2. Formula Weight: 406.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM, Ethanol: 100 mM. SMILES: COCCNC1=NC2=CC=C(C#CC3(O)CCCCC3)C=C2N1C4=NC(N)=NC=C4. InChi Code: InChI=1S/C22H26N6O2/c1-30-14-13-25-21-26-17-6-5-16(7-11-22(29)9-3-2-4-10-22)15-18(17)28(21)19-8-12-24-20(23)27-19/h5-6,8,12,15,29H,2-4,9-10,13-14H2,1H3,(H,25,26)(H2,23,24,27). InChi Key: RZXMIHOUHYSGJO-UHFFFAOYSA-N.