CITCO
CITCO, an imidazothiazole derivative, is a selective agonist of human CAR, with an EC50 value of 49 nM and > 50-fold selectivity to CAR over pregnane X receptor (PXR), and no activity on other nuclear receptors. Upon activation with specific agonists, CAR translocates into the nucleus and binds to the response elements as monomers or CAR/RXR heterodimers. The CAR functions as a xenobiotic receptor, involved in detoxification and clearance of toxic substances from the liver. In addition, activation with selective CAR agonists such as CITCO has also been shown to inhibit growth and expansion of brain tumor stem cells.
Reference:
1. Chakraborty S, Kanakasabai S, Bright JJ. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. British Journal of Cancer, 2011, 104(3): 448-459.
- 1. Liu M, Zhu D, et al. "Berberine Promotes OATP1B1 Expression and Rosuvastatin Uptake by Inducing Nuclear Translocation of FXR and LXRα." Front Pharmacol. 2020;11:375. PMID:32292349
- 2. Hu Q, Yao N, et al. "Constitutive androstane receptor weakens the induction of panaxytriol on CYP3A4 by repressing the activation of pregnane X receptor." Biochem Pharmacol. 2019 Jan;159:32-39. PMID:30414935
| Physical Appearance | A crystalline solid |
| Storage | Desiccate at -20°C |
| M.Wt | 436.74 |
| Cas No. | 338404-52-7 |
| Formula | C19H12Cl3N3OS |
| Solubility | Soluble in DMSO |
| Chemical Name | (E)-6-(4-chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=C(C=C1)C2=C(/C=N/OCC(C=C3Cl)=CC=C3Cl)N4C(SC=C4)=N2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
|
Cell lines |
T98G, U87MG, DB29 and DB33 glioma cells |
|
Reaction Conditions |
2.5 ~ 10 μM CITCO for 48 h incubation |
|
Applications |
The brain tumor stem cells (BTSCs) from T98G and U87MG cultured in the absence of CITCO showed 6.8 and 11% Annexin V-positive cells that increased to 62 and 68% following addition of 10 μM CITCO, respectively. Moreover, BTSCs from DB29 and DB33 gliomas showed 3 and 0.5% Annexin V-positive cells that increased to 24 and 41% following treatment with 10 μM CITCO, respectively. CITCO dose-dependently induced apoptosis in BTSCs in culture, but not in normal astrocytes. |
| Animal experiment:[1] | |
|
Animal models |
Nude mice subcutaneously injected with U87MG–BTSCs |
|
Dosage form |
25 or 100 μg Intraperitoneal injection; on days 22, 24, 26, 30 and 36 |
|
Applications |
CITCO at the dose of 25 μg resulted in a significant decrease in tumour growth, which further decreased to an undetectable level after treatment with 100 μg CITCO. |
|
Note |
The technical data provided above is for reference only. |
|
References: 1. Chakraborty S, Kanakasabai S, Bright JJ. Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. British Journal of Cancer, 2011, 104(3): 448-459. |
|
Quality Control & MSDS
- View current batch:
-
Purity ≥95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
Related Biological Data
Related Biological Data
