2. Apoptosis
  3. Apoptosis
  4. CITCO

CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.

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CITCO Chemical Structure

CITCO Chemical Structure

CAS No. : 338404-52-7

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

CITCO Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CITCO

  • Biological Activity

  • Purity & Documentation

  • References

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Description

CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors[1].

IC50 & Target

CAR, PXR[1]
In Vitro

CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs[1].
CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes[1].
CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes[1].
CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CITCO Related Antibodies

Cell Proliferation Assay[1]

Cell Line: T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes
Concentration: 1, 2.5, 5, 10, 25, 50 μM
Incubation Time: 48 hours
Result: Resulted in a dose-dependent inhibition of viable cell count and proliferation.

Cell Cycle Analysis[1]

Cell Line: The T98G, U87MG, DB29 and DB33 glioma cells
Concentration: 2.5, 5 μM
Incubation Time: 48 hours
Result: Induced cell cycle arrest differentially in different BTSCs in culture.

Apoptosis Analysis[1]

Cell Line: The T98G, U87MG, DB29 and DB33 glioma cells
Concentration: 2.5, 5 or 10 μM
Incubation Time: 48 hours
Result: Increased the levels of Annexin V-positive apoptotic cells in dose dependently.

Western Blot Analysis[1]

Cell Line: T98G, U87MG, DB29 and DB33 glioma cells
Concentration: 0 to 25 μM
Incubation Time: 48 hours
Result: The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.
In Vivo

CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to eight-week-old male athymic nude mice[1]
Dosage: 25 or 100 μg
Administration: Intraperitoneal; on days 22, 24, 26, 30 and 36
Result: Decreased tumour growth.
Molecular Weight

436.74

Formula

C19H12Cl3N3OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(C2=C(/C=N/OCC3=CC=C(Cl)C(Cl)=C3)N4C(SC=C4)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (57.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2897 mL 11.4485 mL 22.8969 mL
5 mM 0.4579 mL 2.2897 mL 4.5794 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.60%

COA (257 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2897 mL 11.4485 mL 22.8969 mL 57.2423 mL
5 mM 0.4579 mL 2.2897 mL 4.5794 mL 11.4485 mL
10 mM 0.2290 mL 1.1448 mL 2.2897 mL 5.7242 mL
15 mM 0.1526 mL 0.7632 mL 1.5265 mL 3.8162 mL
20 mM 0.1145 mL 0.5724 mL 1.1448 mL 2.8621 mL
25 mM 0.0916 mL 0.4579 mL 0.9159 mL 2.2897 mL
30 mM 0.0763 mL 0.3816 mL 0.7632 mL 1.9081 mL
40 mM 0.0572 mL 0.2862 mL 0.5724 mL 1.4311 mL
50 mM 0.0458 mL 0.2290 mL 0.4579 mL 1.1448 mL
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CITCO Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CITCO338404-52-7ApoptosisInhibitorinhibitorinhibit

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