IT-901

SKU: orb1707169

Description

IT-901 is a naphthalene thiobarbiturate derivative that potently and selectively inhibits the NF-κB subunit c-Rel, demonstrating antitumor activity in research models of lymphoma and myeloma. It has been investigated in both in vitro and in vivo studies for its potential in oncology research, particularly for hematological cancers.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1584121-99-2
• MW: 342.37
• Purity: 98.06%
• Formula: C₁₇H₁₄N₂O₄S
• SMILES: C(C=1C2=C(C(OC)=CC1OC)C=CC=C2)=C3C(=O)NC(=S)NC3=O
• Target: Others,NF-κB
• Solubility: DMSO:10 mg/mL (29.21 mM)

Bioactivity

• Target IC50:
  GCB:4 μ M|NF-κB:0.1 μM|c-Rel:2.9μM
• In Vivo:
  Administered intraperitoneally (IP) every other day for 2 weeks at a dose of 24 mg/kg, IT-901 proves to be an effective treatment for acute graft-versus-host disease (GVHD) without compromising its anti-tumor activity. IT-901, given at doses ranging from 12 to 20 mg/kg via IP administration, enhances the pharmacokinetic (PK) profile by increasing both half-life (T1/2) and maximum plasma concentration (Cmax).
• In Vitro:
  Following 24 hours of treatment with IT-901 at concentrations of 1, 3, and 5 μM, there is a reduction in the proliferation of viable ABC and GCB DLBCL cells. At a concentration of 3 μM and a duration of 24 hours, IT-901 induces a dose-dependent decrease in cell viability. However, at least 60 percent of cells remain viable after 48 hours of treatment with 4 μM IT-901 in all tested cell lines, except HBL1. With a treatment duration of 6 hours and concentrations of 1, 5, and 10 μM, IT-901 leads to a diminished expression of p65 and p50 in both nuclear and cytosolic fractions. Additionally, it reduces the expression of the inhibitory subunit IκBα in both 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, while IL-2 secretion is effectively blocked at 5 μM. Concentrations of IT-901 above 10 μM become increasingly toxic and may induce apoptosis in healthy cells. IT-901 demonstrates inhibition of cell growth in both activated B-like (ABC) and germinal center B-like (GCB) cell lines, with IC50 values ranging between 3 μM to 4 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IT 901, IT901, IT-901, NF-κB, c-Rel

Compound Identifiers

PubChem CID

90082813