For research use only. Not for therapeutic Use.
IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD)[1][2].
IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells[1].
IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1[1].
IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines[2].
The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM[1].
The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells[1].
IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC50 values between 3μM to 4μM[1].
IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity[1].
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax[1].
| Catalog Number | I007389 |
| CAS Number | 1584121-99-2 |
| Synonyms | 5-[(2,4-dimethoxynaphthalen-1-yl)methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione |
| Molecular Formula | C17H14N2O4S |
| Purity | ≥95% |
| InChI | 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) |
| InChIKey | JHOPCCOYRKEHQU-UHFFFAOYSA-N |
| SMILES | COC1=CC(=C(C2=CC=CC=C21)C=C3C(=O)NC(=S)NC3=O)OC |
| Reference | [1]. Shono Y, et al. Characterization of a c-Rel Inhibitor That Mediates Anticancer Properties in HematologicMalignancies by Blocking NF-κB-Controlled Oxidative Stress Responses. Cancer Res. 2016 Jan 15;76(2):377-89. [2]. Vaisitti T, et al. Targeting metabolism and survival in chronic lymphocytic leukemia and Richter syndrome cellsby a novel NF-κB inhibitor. Haematologica. 2017 Nov;102(11):1878-1889. |
