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Cat. No.: HY-190705

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TrxR1-IN-5

TrxR1-IN-5 is a thioredoxin reductase 1 (TrxR1) inhibitor. TrxR1-IN-5 covalently and irreversibly inhibits the Sec498 residue in the active site of TrxR1 through a Michael addition reaction, blocking its antioxidant function, thereby inducing intracellular ROS accumulation, mitochondrial membrane potential depolarization, and activation of Bax/Bcl-2-mediated mitochondrial apoptosis. TrxR1-IN-5 can be used for research on non-small cell lung cancer.

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

Formula: C₂₄H₂₁FO₇
Molecular Weight:440.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (289 KB)

TrxR1-IN-5 Chemical Structure

Price

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Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

TrxR1

Bcl-2

Bax

All TrxR Isoforms :

TrxR1
TrxR2

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.92 μM	Cytotoxicity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay. Cytotoxicity against human A549 cells assessed as viability reduction incubated 48 hrs by MTT assay.	42868776
HepG2	IC₅₀	4.95 μM	Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay. Cytotoxicity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.	42868776
MCF7	IC₅₀	3.96 μM	Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay. Cytotoxicity against human MCF-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.	42868776
L02	IC₅₀	10.80 μM	Cytotoxicity against human L-02 cells assessed as viability reduction incubated 48 hrs by MTT assay. Cytotoxicity against human L-02 cells assessed as viability reduction incubated 48 hrs by MTT assay.	42868776

In Vitro

Anti-cancerOxidative StressMitochondrial FunctionApoptosis

Anti-cancer

TrxR1-IN-5 (compound 1g) (48 h) has antiproliferative activity in A549, MCF-7, and HepG2 cells, with IC₅₀ values of 0.92 µM, 3.96 µM, and 4.95 µM, respectively, but has relatively lower cytotoxic activity in normal lung epithelial Beas-2B cells and normal liver epithelial L-02 cells, with IC₅₀ values of 3.79 µM and 10.80 µM, respectively, showing selectivity for A549 ^[1].
TrxR1-IN-5 (2.5-5 µM; 24 h) dose-dependently inhibits intracellular TrxR1 enzyme activity and downregulates TrxR1 protein expression in A549 cells, and its direct target-binding activity is confirmed by CETSA assay^[1].

Oxidative Stress

Mitochondrial Function

Anti-cancer

Apoptosis

TrxR1-IN-5 (2.5-5 µM; 24 h) inhibits cell proliferation, promotes intracellular ROS accumulation, causes mitochondrial membrane potential depolarization, induces apoptosis, downregulates Bcl-2, and upregulates Bax protein expression in A549 cells in a dose-dependent manner^[1].

Oxidative Stress

Mitochondrial Function

Apoptosis

TrxR1-IN-5 (5 µM; 24 h) has the activity of having its induction of ROS accumulation, mitochondrial depolarization, and apoptosis reversed by NAC in A549 cells pretreated with 5 mM NAC (HY-B0215) for 2 h^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A549 cells
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Caused a marked concentration-dependent reduction in EdU-positive A549 cells, with a sharp drop in the EdU-positive ratio at the higher concentration.

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Produced a dose-dependent increase in the proportion of apoptotic A549 cells.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Caused a dose-dependent inhibition of intracellular TrxR1 activity, accompanied by the downregulation of TrxR1 protein expression levels.
Downregulated the expression of anti-apoptotic protein Bcl-2 while upregulating the expression of pro-apoptotic protein Bax.

In Vivo

Anti-cancer

TrxR1-IN-5 (compound 1g) (3.9-15.6 μM; administered in culture medium; single administration; 48 h) significantly inhibits in vivo tumor growth in a concentration-dependent manner in the A549 cell xenograft zebrafish model^[1].

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

Animal Model:

Zebrafish embryos at 2 days post-fertilization (2 dpf) were selected, and human non-small cell lung cancer A549 cells fluorescently labeled with CM-DiI membrane probe were microinjected into the yolk sac of each zebrafish^[1]
Dosage:

3.9 μM, 7.8 μM, 15.6 μM
Administration:

administered in culture medium; single administration; 48 h
Result:

Resulted in a marked and dose-dependent reduction in tumor fluorescence intensity.
Significantly inhibited tumor growth in zebrafish at all tested concentrations, validating its potent anti-tumor efficacy in vivo.

Related Protocols :

Chemical Information

Molecular Weight 440.42
Formula C₂₄H₂₁FO₇
SMILES

O=C1C2=C[C@@H](O1)C[C@](O3)(C)[C@@H]3[C@@H](OC(/C=C/C4=CC=C(F)C=C4)=O)[C@H](C(C(O5)=O)=C)[C@@H]5C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ren H, et al. Novel sesquiterpene lactone derivatives as covalent TrxR1 inhibitors: synthesis, anti-tumor activity, mechanistic investigation. Bioorganic chemistry. 2026 Oct 09;183:110611. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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TrxR1-IN-5

All TrxR Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Description

IC50 & Target

Cellular Effect

In Vitro

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

TrxR1-IN-5 Related Classifications

HY-190705 Related Classifications

Bioz

Keywords

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