2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Autophagy
  3. TrxR Reactive Oxygen Species (ROS) Autophagy Atg8/LC3 Beclin1 p62
  4. TrxR-IN-2

TrxR-IN-2 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 increases reactive oxidative species (ROS) levels and decreases mitochondrial transmembrane potential levels. TrxR-IN-2 triggers DNA damage via H2AX regulation, and induces autophagy via LC3, beclin-1, and p62 regulation. TrxR-IN-2 can be used for the research of drug-resistant hepatocellular carcinoma[1].

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

TrxR-IN-2

TrxR-IN-2 Chemical Structure

CAS No. : 2866261-50-7

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TrxR-IN-2 Related Antibodies

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Description

TrxR-IN-2 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 increases reactive oxidative species (ROS) levels and decreases mitochondrial transmembrane potential levels. TrxR-IN-2 triggers DNA damage via H2AX regulation, and induces autophagy via LC3, beclin-1, and p62 regulation. TrxR-IN-2 can be used for the research of drug-resistant hepatocellular carcinoma[1].

Cellular Effect
Cell Line Type Value Description References
Bel-7402 IC50
0.8 μM
Compound: 11
Antiproliferative activity against human Bel-7402 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human Bel-7402 cells incubated for 24 hrs by MTT assay
[PMID: 34806369]
Bel7402/5-FU IC50
0.9 μM
Compound: 11
Antiproliferative activity against human BEL-7402/5-FU cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human BEL-7402/5-FU cells incubated for 24 hrs by MTT assay
[PMID: 34806369]
HGC-27 IC50
1.4 μM
Compound: 11
Antiproliferative activity against human HGC-27 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells incubated for 24 hrs by MTT assay
[PMID: 34806369]
HepG2 IC50
1.1 μM
Compound: 11
Antiproliferative activity against human HepG2 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated for 24 hrs by MTT assay
[PMID: 34806369]
In Vitro

TrxR-IN-2 (Compound 11) (72 h) potently inhibits the proliferation of Bel7402, HepG2, HGC27, and Bel-7402/5-FU cells with IC50 values ranging from 0.8 μM to 1.4 μM[1].
TrxR-IN-2 (0.2 μM) potently inhibits TrxR activity in Bel-7402/5-FU cells with an IC50 of 0.2 μM[1].
TrxR-IN-2 (0.3-3.0 μM; 24 h) induces dose-dependent ROS accumulation in Bel-7402/5-FU cells[1].
TrxR-IN-2 (1-10 μM) significantly reduces mitochondrial transmembrane potential in Bel-7402/5-FU cells[1].
TrxR-IN-2 (1.0-3.0 μM; 72 h) triggers DNA damage in Bel-7402/5-FU cells by up-regulating the expression of H2AX.S139ph, p-p53, and p53[1].
TrxR-IN-2 (1.0-3.0 μM; 24 h) induces dose-dependent autophagosome formation in Bel-7402/5-FU cells[1].
TrxR-IN-2 (0.3-3.0 μM; 72 h) triggers autophagy in Bel-7402/5-FU cells by dose-dependently increasing the LC3-II/LC3-I ratio and beclin-1 expression, and decreasing p62 expression[1].

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

TrxR-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Bel-7402/5-FU drug-resistant human liver carcinoma cells
Concentration: 1.0 μM; 3.0 μM
Incubation Time: 72 h
Result: Increased the expression of DNA damage biomarker H2AX.S139ph, phosphorylated p53 (p-p53), and total p53 in a dose-dependent manner.

Cell Autophagy Assay[1]

Cell Line: Bel-7402/5-FU drug-resistant human liver carcinoma cells
Concentration: 1.0 μM; 3.0 μM
Incubation Time: 24 h
Result: Induced autophagosome formation in a dose-dependent manner; at 3.0 μM, triggered autophagy more pronouncedly than piperlongumine at the same concentration.

Western Blot Analysis[1]

Cell Line: Bel-7402/5-FU drug-resistant human liver carcinoma cells
Concentration: 0.3 μM; 1.0 μM; 3.0 μM
Incubation Time: 72 h
Result: Up-regulated the conversion of LC3-I to LC3-II (increasing the LC3-II/LC3-I ratio in a dose-dependent manner) and the expression of beclin-1, while down-regulating the expression of p62.
Was more potent than piperlongumine in modulating these protein levels.
In Vivo

TrxR-IN-2 (Compound 11) (60-303.8 mg/kg; i.p.; single dose) has an intraperitoneal LD50 of 178 mg/kg in female ICR mice[1].
TrxR-IN-2 (2-5 mg/kg; i.p.; 21 days) exhibits potent in vivo antitumor activity in Bel-7402/5-FU xenograft nude mice[1].

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

Animal Model: ICR mice (female)[1]
Dosage: 60.0 mg/kg; 90.0 mg/kg; 135.0 mg/kg; 202.5 mg/kg; 303.8 mg/kg
Administration: i.p.; single dose
Result: Achieved 100% survival of mice 14 days post-administration at 60.0 mg/kg.
Achieved 90% survival of mice 14 days post-administration at 90.0 mg/kg.
Achieved 60% survival of mice 14 days post-administration at 135.0 mg/kg.
Achieved 30% survival of mice 14 days post-administration at 202.5 mg/kg.
Achieved 10% survival of mice 14 days post-administration at 303.8 mg/kg.
Calculated a median lethal dose (LD50) of 178 mg/kg.
Animal Model: Nude mice (Bel-7402/5-FU xenograft tumor model)[1]
Dosage: 2 mg/kg; 5 mg/kg
Administration: i.p.; 21 days
Result: Significantly suppressed tumor growth compared to the control group at 2 mg/kg, reducing mean tumor weight to ~0.7 g.
Suppressed tumor growth by 76% compared to the control group at 5 mg/kg, reducing mean tumor weight to ~0.45 g.
Showed greater tumor growth inhibition than the 5 mg/kg dose of piperlongumine at 5 mg/kg.
Molecular Weight

406.43

Formula

C22H22N4O4
CAS No.
SMILES

O=C1C=CCCN1C(/C=C/C2=NC(C)=C(/C=C/C(N3CCC=CC3=O)=O)N=C2C)=O
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TrxR-IN-2 Related Classifications

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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:

TrxR-IN-22866261-50-7TrxRReactive Oxygen Species (ROS)AutophagyAtg8/LC3Beclin1p62Thioredoxin ReductaseAutophagy-related 8Atg6Sequestosome-1SQSTM1Bel-7402/5-FUdrug-resistant cancer cellsBel7402ICR miceselenocysteineHepG2reactive oxidative speciesdrug-resistant hepatocellular carcinomaHGC27thioredoxin reductaseInhibitorinhibitorinhibit

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