IT-901

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IT-901 是一种新型强效小分子 NF-κB 亚基 c-Rel 抑制剂。

IT-901 is a novel potent, small molecule inhibitor of NF-κB subunit c-Rel, inhibits DNA binding of c-Rel and NF-κB activity with IC50 of 3 uM; reduces stimulation of the oxidative stress response gene heme oxygenase-1, inhibits c-Rel/NF-κB both in vitro and in vivo.

IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells. 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. 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. The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM. The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells. 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. Cell Proliferation Assay Cell Line:TMD8 and SU-DHL8 cells Concentration:1, 3, 5 μM.Incubation Time:For 24 hours Result:Resulted in decreased proliferation of viable ABC and GCB DLBCL cells.Cell Viability Assay Cell Line:SU-DHL8 and TMD8 cells.Concentration:3 μM Incubation Time:For 24 hours Result:Decreased cell viability in a dose-dependent fashion.Western Blot Analysis Cell Line:Primary chronic lymphocytic leukemia (CLL) cells and cell lines.Concentration:1, 5, 10 μM.Incubation Time:For 6 hours Result:Documented Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreased the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms.

IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity. IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax. Animal Model:BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old Dosage:24 mg/kg Administration:IP; every other day for 2 weeks Result:Had an effective treatment of acute GVHD without impairing anti-tumor activity.

IT 901 | IT901

Apoptosis

NF-κB

NF-κB

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1584121-99-2

342.37

C17H14N2O4S

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (36.51 mM)

O=C(/C(C(N1)=O)=C\C2=C3C=CC=CC3=C(OC)C=C2OC)NC1=S

5-[(2,4-dimethoxy-1-naphthalenyl)methylene]dihydro-2-thioxo-4,6(1H,5H)-pyrimidinedione

(-20℃)

With Ice Pack

≥ 2 years