CITCO
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
T98G, U87MG, DB29 and DB33 glioma cells |
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Reaction Conditions |
2.5 ~ 10 μM CITCO for 48 h incubation |
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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] | |
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Animal models |
Nude mice subcutaneously injected with U87MG–BTSCs |
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Dosage form |
25 or 100 μg Intraperitoneal injection; on days 22, 24, 26, 30 and 36 |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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化学结构
相关生物数据
相关生物数据
