IT-901

IT-901 is an inhibitor of the NF-κB subunit c-Rel.¹ It inhibits NF-κB DNA binding in HBL1 cells (IC₅₀ = 0.1 µM) and reduces TNF-α-induced NF-κB 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; Item No. 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.^1,2

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1. Shono, Y., Tuckett, A.Z., Liou, H.-C., et al. Characterization of a c-Rel inhibitor that mediates anticancer properties in hematologic malignancies by blocking NF-κB-controlled oxidative stress responses. Cancer Res. 76(2), 377-389 (2016).

2. Vaisitti, T., Gaudino, F., Ouk, S., et al. Targeting metabolism and survival in chronic lymphocytic leukemia and Richter syndrome cells by a novel NF-κB inhibitor. Haematologica 102(11), 1878-1889 (2017).