1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Tetrahydrouridine

Tetrahydrouridine  (Synonyms: THU; NSC-112907)

Cat. No.: HY-15345A Purity: 99.89%
Handling Instructions Technical Support

Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

For research use only. We do not sell to patients.

Tetrahydrouridine Chemical Structure

Tetrahydrouridine Chemical Structure

CAS No. : 18771-50-1

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Tetrahydrouridine:

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Description

Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[1][2].

IC50 & Target

Cytidine deaminase (CDA)[1]

In Vitro

Tetrahydrouridine (THU) is a specific inhibitor of cytidine deaminase (CDA) which can suppress deamination in the catabolism of cytotoxic deoxycytidine analogues like ara-C and Gemcitabine. To test how Tetrahydrouridine affects the Gemcitabine-mediated anti-neoplastic effect on pancreatic and lung carcinoma cells, a combination therapy is performed. As expected, high CDA expression in BxPC-3 and H441 results in improved Gemcitabine sensitivity after a 100 μM Tetrahydrouridine treatment. The sensitivity of BxPC-3 and H441 cell lines increases by as much as approximately 2.1 and 4.4 fold respectively. On the other hand, MIAPaCa-2 and H1299 cells unexpectedly become more sensitive to Gemcitabine with low CDA expression. MIAPaCa-2 and H1299 cells show a change in IC50 of 2.2 and 2.3 fold respectively. However, Panc-1 and H322 cells do not show significant changes in drug sensitivity. These data suggested that Tetrahydrouridine can sensitize some pancreatic and lung carcinoma cells to Gemcitabine-induced cell death regardless of CDA expression levels. Tetrahydrouridine inhibits S-phase without apoptosis[1].

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

In Vivo

Administration of 167 mg/kg Tetrahydrouridine (THU) followed by 1.0 mg/kg DAC results in death in one male and eight females. Animals surviving to scheduled termination are generally asymptomatic with no treatment related effects observed in body weights, food consumption, clinical chemistry and urinalysis for a treatment up to 1.0 mg/kg DAC in combination with 167 mg/kg Tetrahydrouridine in animals[2].

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

Clinical Trial
Molecular Weight

248.23

Formula

C9H16N2O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N([C@H]2[C@H](O)[C@H](O)[C@@H](CO)O2)CCC(O)N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (402.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0285 mL 20.1426 mL 40.2852 mL
5 mM 0.8057 mL 4.0285 mL 8.0570 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.89%

References
Cell Assay
[1]

Cell growth for pancreatic and lung carcinoma cell lines is carried out using the colorimetric methylene blue assay in 96-well plates at a density of 5,000 cells/well. Cells are either exposed or not exposed to Tetrahydrouridine (100 µM), counting the first 12 hrs as Day 0. Mean values are calculated from three different wells in triplicates for four days[1].

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

Animal Administration
[2]

Mice[2]
CD-1 mice (male 30-38 g and female 24-31g) from are individually housed in polycarbonate cages suspended on stainless steel racks with SaniChip certified hardwood bedding. Mice are assigned to four dose groups and a vehicle control group. Animals are gavaged with DAC or its vehicle 1 hour ± 5 minutes after administration of THU or its vehicle at a dose volume of 10 mL/kg. The DAC doses are selected based on the range finding study in which the mice tolerated six oral doses (2x/week) of 0.1, 0.2 and 0.4 mg/kg DAC in combination with a fixed dose of 167 mg/kg THU. A fixed Tetrahydrouridine dose (500 mg/m2) and the optimal timing between Tetrahydrouridine and DAC administration (60 min) are selected. Conversion of milligrams per body surface area dose in mice into milligrams per kilogram body weight dose estimation is based on Michaelis constant (km) values for mice obtained from US Food and Drug Administration published guidelines. In brief, the mouse dose in milligrams per body surface area (500 mg/m2) is divided by the km of 3 to convert the dose to milligrams per kilogram body weight (167 mg/kg).

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

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. 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
H2O 1 mM 4.0285 mL 20.1426 mL 40.2852 mL 100.7131 mL
5 mM 0.8057 mL 4.0285 mL 8.0570 mL 20.1426 mL
10 mM 0.4029 mL 2.0143 mL 4.0285 mL 10.0713 mL
15 mM 0.2686 mL 1.3428 mL 2.6857 mL 6.7142 mL
20 mM 0.2014 mL 1.0071 mL 2.0143 mL 5.0357 mL
25 mM 0.1611 mL 0.8057 mL 1.6114 mL 4.0285 mL
30 mM 0.1343 mL 0.6714 mL 1.3428 mL 3.3571 mL
40 mM 0.1007 mL 0.5036 mL 1.0071 mL 2.5178 mL
50 mM 0.0806 mL 0.4029 mL 0.8057 mL 2.0143 mL
60 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6786 mL
80 mM 0.0504 mL 0.2518 mL 0.5036 mL 1.2589 mL
100 mM 0.0403 mL 0.2014 mL 0.4029 mL 1.0071 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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.

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Tetrahydrouridine
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