TRi-1

Name: TRi-1
Brand: MedChemExpress
SKU: HY-125006
Rating: 5.0 (5 reviews)

Cat. No.: HY-125006 Purity: 99.69%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 246020-68-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE TRi-1

Bio/Physico-chemical Assay

In Vivo Efficacy Study

IHC

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; Immunoblot of the indicated protein in control proliferating and oncogenic RAS-induced senescent IMR90 cells with or without TXNRD1 knockdown or treatment with a pharmacological TXNRD1 inhibitor Tri-1 (5 μM).

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; Immunostaining for cGAS and γH2AX in oncogenic RAS-induced senescent IMR90 cells treated with vehicle control or TXNRD1 inhibitor Tri-1 (5 μM).

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; Enrichment of the SASP genes among genes that were significantly downregulated by both TXNRD1 knockdown and TXNRD1 inhibitor Tri-1 treatment in oncogenic RAS-induced senescent IMR90 cells determined by RNA-seq analysis.

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; GST pull-down assay using purified His-cGAS and GST-TXNRD1 with or without Tri-1 (1 hr before cGAS addition) or auranofin in the reaction. GST was used a negative control.

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; Tumor growth stimulated by co-injected senescent IMR90 fibroblasts in a xenograft mouse model was inhibited by TXNRD1 knockdown or Tri-1 (10 mg/kg, once every 3 days, ip) treatment. TOV21G cells were subcutaneously injected with the indicated senescent IMR90 cells into NSG female mice. The tumor weight was measured at the end of the experiment.

: TRi-1 purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Feb;4(2):185-197. [Abstract]; Images of immunostaining for NLRP3 in the ovary tissues from young (4 months) and aged mice (22 months) with or without Tri-1 and auranofin treatments.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

246020-68-8

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
10 mM	0.3042 mL	1.5210 mL	3.0420 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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: 99.69%

Select Batch:

Data Sheet (280 KB) SDS (394 KB)

COA (252 KB) HNMR (237 KB) RP-HPLC (260 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Stafford WC, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444. [Content Brief]

Complete Stock Solution Preparation Table

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

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 1p38 MAPKJNKc-Jun N-terminal kinaseglutathioneTXNRD1thioredoxin reductase 1FaDuantitumorInhibitorinhibitorinhibit

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TRi-1

Customer Review

TRi-1 Related Antibodies

5 Publications Citing Use of MCE TRi-1

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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Biological Activity

Purity & Documentation

References

Customer Review

TRi-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TRi-1 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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SAFETY DATA SHEET (SDS)

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