TOP1210 is superior to selective kinase inhibitors alone in downregulating proinflammatory cytokine release from UC biopsies. TOP1210 activity is comparable to a combination of all three selective inhibitors and reduces proinflammatory cytokine release from UC biopsies in a concentration-dependent manner. Effect of 1 μg/mL TOP1210, 1 μg/mL BIRB-796 (BIRB), 1 μg/mL dasatinib (DAS), and 1 μg/mL BAY-61-3606 (BAY), or the combination of the 3 selective kinase inhibitors (A) or TOP1210 (0.001–1 μg/mL) (B) on the release of IL-1β, IL-6, and IL-8, expressed as mean percent inhibition compared with control (DMSO; DMSO, 0.5% v/v), in organ culture supernatants of inflamed colonic biopsies from patients with UC. Bars represent mean ± SEM of at least 3 independent experiments. *P < 0.05 versus DMSO; **P < 0.005 versus DMSO; ***P < 0.0005 versus DMSO.