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TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.

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TRi-1 Chemical Structure

TRi-1 Chemical Structure

CAS No. : 246020-68-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
1 mg USD 85 In-stock
5 mg USD 180 In-stock
10 mg USD 280 In-stock
50 mg USD 650 In-stock
100 mg USD 950 In-stock
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Based on 2 publication(s) in Google Scholar

TRi-1 Related Antibodies

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Description

TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy[1].

IC50 & Target

IC50: 12 nM (TXNRD1)[1].
In Vitro

TRi-1 (0.679 and 6.79 μM; 6 h) has no effect on cellular glutathione (GSH) concentrations in FaDu cells, efficiently activates JNK and p38 phosphorylation[1].
TRi-1 (2 μM) irreversibly inhibit TXNRD1 in an NADPH-dependent manner[1].
TRi-1 (0.1-10 μM; 0-10 h) increases cellular H2O2 production in cultured FaDu cells in a concentration- and time-dependent manner[1].
TRi-1 (10 nM-100 μM; 48 h) shows cytotoxicity toward cancer cells[1].

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

TRi-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: FaDu cells
Concentration: 0.679 and 6.79 μM
Incubation Time: 6 h
Result: Efficiently activated JNK and p38 phosphorylation.

Cell Cytotoxicity Assay[1]

Cell Line: Leukemia, non-small cell lung, CNS, colon, melanoma, ovarian, renal, prostate and breast cancer cells
Concentration: 10 nM-100 μM
Incubation Time: 48 h
Result: Displayed potency against every cell line tested, with an average growth inhibition to 50% (GI50) of 6.31 μM.
In Vivo

TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors[1].

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

Animal Model: SCID mice bearing established human FaDu cell xenografts[1]
Dosage: 10 mg/kg
Administration: Intravenous injection, twice a day for 4 days
Result: Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.
Animal Model: PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, twice a week for 3 weeks
Result: Impaired tumor growth, significantly reduced tumor volumes.
Molecular Weight

328.73

Formula

C12H9ClN2O5S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=[N+](C1=CC=C(OC)N=C1S(=O)(C2=CC=C(Cl)C=C2)=O)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (190.13 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 3.0420 mL 15.2100 mL 30.4201 mL
5 mM 0.6084 mL 3.0420 mL 6.0840 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 (protect from light). 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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  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

SDS (393 KB)

COA (252 KB) HNMR (236 KB) RP-HPLC (244 KB) LCMS (93 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 (protect from light). 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 3.0420 mL 15.2101 mL 30.4201 mL 76.0503 mL
5 mM 0.6084 mL 3.0420 mL 6.0840 mL 15.2101 mL
10 mM 0.3042 mL 1.5210 mL 3.0420 mL 7.6050 mL
15 mM 0.2028 mL 1.0140 mL 2.0280 mL 5.0700 mL
20 mM 0.1521 mL 0.7605 mL 1.5210 mL 3.8025 mL
25 mM 0.1217 mL 0.6084 mL 1.2168 mL 3.0420 mL
30 mM 0.1014 mL 0.5070 mL 1.0140 mL 2.5350 mL
40 mM 0.0761 mL 0.3803 mL 0.7605 mL 1.9013 mL
50 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5210 mL
60 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2675 mL
80 mM 0.0380 mL 0.1901 mL 0.3803 mL 0.9506 mL
100 mM 0.0304 mL 0.1521 mL 0.3042 mL 0.7605 mL
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TRi-1 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:

TRi-1246020-68-8TRi1TRi 1OthersglutathioneTXNRD1thioredoxin reductase 1FaDuantitumorInhibitorinhibitorinhibit

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