(E/Z)-IT-603

(E/Z)-IT-603 is a c-Rel inhibitor (IC50 = 3 µM). It inhibits c-Rel DNA binding to the IL2 promoter in an EMSA. (E/Z)-IT-603 reduces the proliferation of OCI-Ly3 diffuse large B cell lymphoma cells (IC50 = 18 µM). It reduces Huh7 epithelial carcinoma spheroid growth when used at a concentration of 20 µM in combination with the anthracycline antitumor antibiotic doxorubicin (Cay-15007). Preincubation of (E/Z)-IT-603 (20 µM) with murine T cells co-administered with A20 murine lymphoma cells to lethally irradiated mice as a model of T cell-depleted bone marrow transplantation reduces allo-stimulation without affecting anticancer T cell responses and increases survival. In vivo, (E/Z)-IT-603 (24 mg/kg every other day), when used in combination with doxorubicin, reduces hepatic tumor burden, increases CD8+ T cell and F4/80+ macrophage tumor infiltrates, and increases tumoral mRNA encoding chemokine (C-X-C motif) ligand 9 (Cxcl9) in a Hep-53.4 murine hepatocellular carcinoma model.Formal Name: 5-[(5-bromo-2-hydroxy-3-methoxyphenyl)methylene]-2-thioxo-4-imidazolidinone. CAS Number: 292168-90-2. Molecular Formula: C11H9BrN2O3S. Formula Weight: 329.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C1NC(NC1=CC2=C(O)C(OC)=CC(Br)=C2)=S. InChi Code: InChI=1S/C11H9BrN2O3S/c1-17-8-4-6(12)2-5(9(8)15)3-7-10(16)14-11(18)13-7/h2-4,15H,1H3,(H2,13,14,16,18). InChi Key: PYLYAEDUIKQBOT-UHFFFAOYSA-N.