RBN-012759

RBN-012759 is an inhibitor of poly(ADP-ribose) polymerase 14 (PARP14, IC50 = 0.003 µM). It is selective for PARP14 over PARP1-4, -5a, -5b, -6-12, -15, and -16 (IC50s = 1->100 µM). RBN-012759 (10 µM) inhibits IFN-gamma-induced PARP14 auto-MARylation in CFPAC-1 cells. It inhibits IL-4-induced protumor M2-like macrophage polarization in isolated human primary macrophages. RBN-012759 (1 µM) also induces expression of the genes encoding the pro-inflammatory chemokines chemokine (C-C motif) ligand 13 (CCL13), CCL19, and chemokine (C-X-C motif) ligand 11 (CXCL11) in human kidney cancer tumor explants.Formal Name: 7-(cyclopropylmethoxy)-5-fluoro-2-[[(trans-4-hydroxycyclohexyl)thio]methyl]-4(3H)-quinazolinone. CAS Number: 2360851-29-0. Molecular Formula: C19H23FN2O3S. Formula Weight: 378.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 243 nm. SMILES: FC1=C2C(NC(CS[C@@H]3CC[C@H](CC3)O)=NC2=O)=CC(OCC4CC4)=C1. InChi Code: InChI=1S/C19H23FN2O3S/c20-15-7-13(25-9-11-1-2-11)8-16-18(15)19(24)22-17(21-16)10-26-14-5-3-12(23)4-6-14/h7-8,11-12,14,23H,1-6,9-10H2,(H,21,22,24)/t12-,14-. InChi Key: NKZDEFKPZSLQRF-MQMHXKEQSA-N.