IT-901

IT-901 is an inhibitor of the NF-kappaB subunit c-Rel. It inhibits NF-kappaB DNA binding in HBL1 cells (IC50 = 0.1 µM) and reduces TNF-alpha-induced NF-kappaB activity in a reporter assay (IC50 = 4 µM). IT-901 decreases proliferation of activated B-like (ABC) and germinal center B-like (GCB) human diffuse large B cell lymphoma (DLBCL) cells when used at a concentration of 3 µM. It increases the expression of heme oxygenase-1 (HO-1, Cay-22731) in DLBCL cells and increases the production of reactive oxygen species (ROS) in the mitochondria of DLBCL cells but not normal leukocytes. IT-901 increases survival in a mouse model of graft versus host disease (GVHD) when administered at a dose of 24 mg/kg every other day beginning eight days after hematopoietic stem cell transplantation (HSCT). It also reduces tumor growth in mouse xenograft models of B cell lymphoma induced by Epstein-Barr virus (EBV), chronic lymphocytic leukemia (CLL), and Richter syndrome.Formal Name: 5-[(2,4-dimethoxy-1-naphthalenyl)methylene]dihydro-2-thioxo-4,6(1H,5H)-pyrimidinedione. CAS Number: 1584121-99-2. Molecular Formula: C17H14N2O4S. Formula Weight: 342.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 240, 286, 331, 493 nm. SMILES: S=C(N1)NC(/C(C1=O)=C\C2=C(OC)C=C(OC)C3=C2C=CC=C3)=O. InChi Code: InChI=1S/C17H14N2O4S/c1-22-13-8-14(23-2)11(9-5-3-4-6-10(9)13)7-12-15(20)18-17(24)19-16(12)21/h3-8H,1-2H3,(H2,18,19,20,21,24). InChi Key: JHOPCCOYRKEHQU-UHFFFAOYSA-N.