CID-2858522

SKU: orb1296065

Description

CID-2858522 is a potent small molecule inhibitor of antigen receptor-mediated NF-κB activation, exhibiting an IC50 of 70 nM. It serves as a valuable research tool for studying NF-κB signaling in immunology and inflammation, with applications in both cellular and biochemical assays.

Research Area

Signal Transduction

Key Properties

• CAS Number: 758679-97-9
• MW: 465.63
• Purity: 96.12% (May vary between batches)
• Formula: C₂₈H₃₉N₃O₃
• SMILES: Cc1cc2nc(NCCCO)n(CC(=O)c3cc(c(O)c(c3)C(C)(C)C)C(C)(C)C)c2cc1C
• Target: NF-κB
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.15 mM);DMSO:6.5 mg/mL (13.96 mM)

Bioactivity

• Target IC50:
  NF-κB:70 nM
• In Vivo:
  CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose .
  Read more...
• In Vitro:
  CID-2858522 (Compound 1) also inhibits testosterone hydroxylase in the presence of human liver microsomes and an NADPH generating system (IC50: 85 μM) . In the HEK293 cell line, CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner, with IC50 ~70 nM and with maximum inhibition achieved at 0.25-0.5 μM. In contrast, CID-2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4 μM. CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays .
  Read more...
• Cell Research:
  Cell viability is estimated based on cellular ATP levels. HEK293 cells at a density of 10^5/mL are seeded at 90 μL per well in 96-well white plates and cultured overnight. Compounds (e.g., CID-2858522; 1 μM, 2 μM, 3 μM, and 4 μM) are added (5 μL in medium) to wells and cells are cultured for 16 h, Finally, 50 μL ATPlite solution is added to each well and luminescence activity is read using a luminometer .
  Read more...
• Animal Research:
  Three male mice are subjected to CID-2858522 (single i.p doses at 10, 30, and 50 mg/kg). Blood is drawn at 0.5 and 3 h, and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522 .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CID 2858522, CID2858522, CID-2858522, inhibit, Nuclear factor-kappaB, Nuclear factor-κB, NF-kB, NFκB, NF-κB, NFkB, Inhibitor

Compound Identifiers

PubChem CID

2858523