IT-901 is an orally active and potent inhibitor of the NF-κB subunit c-Rel, with IC50 values of 0.1 µM for NF-κB DNA binding and 3 μM for c-Rel DNA binding, respectively. As a bioactive naphthalenethiobarbiturate derivative, IT-901 holds promise for treating human lymphoid tumors and alleviating graft-versus-host disease (GVHD) [1][2].
体内研究
IT-901 (24 mg/kg; IP; every other day for 2 weeks) effectively treats acute graft-versus-host disease (GVHD) without compromising anti-tumor activity [1].
IT-901(12-20 mg/kg; IP) enhances the pharmacokinetic profile by elevating T1/2 and Cmax [1].
体外研究
IT-901 (1, 3, 5 μM; for 24 hours) leads to reduced proliferation of viable ABC and GCB DLBCL cells [1].
IT-901 (at 3 μM for 24 hours) reduces cell viability in a dose-dependent manner, with at least 60 percent of cells remaining viable after 48 hours of treatment with IT-901 (4 μM) in all tested cell lines except HBL1 [1].
IT-901 (1, 5, 10 μM; for 6 hours) results in reduced expression of p65 and p50 in both nuclear and cytosolic fractions, along with decreased expression of the inhibitory subunit IκBα in phosphorylated and non-phosphorylated forms in primary CLL cells [2].
The IC50 of IT-901/GDM-12 for c-Rel is 2.9 μM, while IL-2 secretion is effectively inhibited at 5 μM [1].
Concentrations of IT-901 exceeding 10 μM progressively induce toxicity and may trigger apoptosis in healthy cells [1].
IT-901 suppresses cell growth in both activated B-like (ABC) and germinal center B-like (GCB) cell lines, with IC50 values ranging from 3μM to 4μM [1].
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