CITCO

SKU: orb1308447

Description

CITCO is a selective agonist of the constitutive androstane receptor (CAR) and an inhibitor of the pregnane X receptor (PXR) with an EC50 of 49 nM. This imidazothiazole derivative suppresses brain tumor stem cell (BTSC) proliferation and is utilized in vitro and in vivo to study nuclear receptor signaling in oncology and toxicology.

Research Area

Cell Biology

Key Properties

• CAS Number: 338404-52-7
• MW: 436.74
• Purity: 99.62% (May vary between batches)
• Formula: C₁₉H₁₂Cl₃N₃OS
• SMILES: C(=NOCC1=CC(Cl)=C(Cl)C=C1)C2=C(N=C3N2C=CS3)C4=CC=C(Cl)C=C4
• Target: Apoptosis
• Solubility: DMSO:11 mg/mL (25.19 mM);H2O:insoluble;10% DMSO+90% Corn Oil:1 mg/mL (2.29 mM)

Bioactivity

• In Vivo:
  CITCO (intraperitoneal; 25 μg; on days 22, 24, 26, 30 and 36) results a significant decrease in tumour growth. After treatment with 100 μg CITCO, it further decreases to an undetectable level .
• In Vitro:
  CITCO (1-50 μM; 48 hours) results in dose-dependent inhibition of viable cell count and proliferation in T98G, U87MG glioma, and BTSCs. CITCO (0-25 μM; 48 hours) significantly increases CAR protein expression in T98G, U87MG glioma, and BTSCs. CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in a dose-dependent manner, but not in normal astrocytes. CITCO (2.5, 5 μM; 48 hours) induces differential cell cycle arrest in various BTSCs in culture, but not in normal astrocytes.

Storage & Handling

• Storage: store at low temperature | 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

PXR, inhibit, Inhibitor, CITCO, Apoptosis, CAR

Compound Identifiers

PubChem CID

3751173