2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. TrxR Reactive Oxygen Species (ROS) Apoptosis Caspase
  4. TrxR2-IN-1

TrxR2-IN-1 is a thioredoxin reductase 2 (TrxR2) inhibitor with an IC50 value of 0.83 μM. TrxR2-IN-1 accumulates in mitochondria, impairs mitochondrial function and membrane potential, increases reactive oxygen species (ROS) levels, activates ASK1-mediated caspase-dependent apoptosis (apoptosis), induces G2/M cell cycle arrest, and inhibits cancer cell migration. TrxR2-IN-1 can be used in the research of hepatocellular carcinoma.

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

TrxR2-IN-1

TrxR2-IN-1 Chemical Structure

CAS No. : 3085154-16-8

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TrxR2-IN-1 Related Antibodies

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Description

TrxR2-IN-1 is a thioredoxin reductase 2 (TrxR2) inhibitor with an IC50 value of 0.83 μM. TrxR2-IN-1 accumulates in mitochondria, impairs mitochondrial function and membrane potential, increases reactive oxygen species (ROS) levels, activates ASK1-mediated caspase-dependent apoptosis (apoptosis), induces G2/M cell cycle arrest, and inhibits cancer cell migration. TrxR2-IN-1 can be used in the research of hepatocellular carcinoma[1].

IC50 & Target[1]

TrxR2

0.83 μM ()

In Vitro

TrxR2-IN-1 (Compound 23d) (48 h) potently inhibits the viability of A549, HCT116, HeLa, Huh7 and MDA-MB-231 cancer cells, and exhibits high selectivity toward normal HHL5 hepatocytes; its IC50 is 0.19 μM and SI is 15.24 in Huh7 cells[1].
TrxR2-IN-1 (0.8-1.6 μM; 24 h) induces dose-dependent morphological changes in Huh7 cells, which indicate inhibited cell growth and the occurrence of cell death[1].
TrxR2-IN-1 (0.8-1.6 μM; 24 h) inhibits the migration of Huh7 cells in a dose-dependent manner[1].
TrxR2-IN-1 (0.4-1.6 μM; 24 h) induces dose-dependent G2/M phase arrest in Huh7 cells[1].
Antitumor agent-215 (0.4-1.6 μM; 24 h) induces apoptosis in Huh7 cells in a dose-dependent manner[1].
Antitumor agent-215 (0.8-1.6 μM; 24 h) induces dose-dependent mitochondrial membrane potential disruption in Huh7 cells[1].
Antitumor agent-215 (0.8-1.6 μM; 24 h) dose-dependently increases the levels of total reactive oxygen species (ROS) and mitochondrial superoxide in Huh7 cells[1].
TrxR2-IN-1 (1.6 μM; 24 h) accumulates in the mitochondria of Huh7 cells at a level 2.6-fold higher than that of its non-targeted precursor 4d[1].
TrxR2-IN-1 (0.4-1.6 μM; 24 h) dose-dependently activates the ASK1-mediated caspase apoptotic pathway in Huh7 cells, and upregulates the levels of phosphorylated ASK1, cleaved caspase-9 and cleaved caspase-3[1].

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

TrxR2-IN-1 Related Antibodies

Cell Migration Assay[1]

Cell Line: Huh7
Concentration: 0.8 μM; 1.6 μM
Incubation Time: 24 h
Result: Reduced cell migration to 77.5% of the control group at 0.8 μM.
Reduced migration to 70.5% of the control group at 1.6 μM, showing a dose-dependent inhibitory effect.

Cell Cycle Analysis[1]

Cell Line: Huh7
Concentration: 0.4 μM; 0.8 μM; 1.6 μM
Incubation Time: 24 h
Result: Caused a dose-dependent accumulation of cells in the G2/M phase, increasing from 28.2% in the control group to 39.0% at 1.6 μM.
Induced corresponding decreases in G1 and S phase cell proportions.

Apoptosis Analysis[1]

Cell Line: Huh7, HHL5
Concentration: 0.4 μM; 0.8 μM; 1.6 μM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in apoptotic cell populations in Huh7 cells, reaching 11.9%, 22.3%, and 46.6% at 0.4, 0.8, and 1.6 μM respectively.
Caused only a slight increase in apoptotic population in HHL5 cells, from 1.0% to 3.2% at 1.6 μM, showing selective pro-apoptotic activity in cancer cells.

Western Blot Analysis[1]

Cell Line: Huh7
Concentration: 0.4 μM; 0.8 μM; 1.6 μM
Incubation Time: 24 h
Result: Caused a dose-dependent increase in the ratio of p-ASK1/ASK1, cleaved-caspase-9/caspase-9, and cleaved-caspase-3/caspase-3, indicating activation of the ASK1-mediated caspase apoptosis cascade.
In Vivo

TrxR2-IN-1 (Compound 23d) (1.25-5 mg/kg; subcutaneous injection; every 2 days for 14 days) exhibits potent, dose-dependent antitumor activity in a Huh7 hepatocellular carcinoma xenograft model[1].

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

Animal Model: BALB/cA-nude (female, 5-6 weeks old, 19−21 g, subcutaneous inoculation of Huh7 cells)[1]
Dosage: 1.25 mg/kg; 2.5 mg/kg; 5 mg/kg
Administration: subcutaneous injection; every 2 days for 14 days
Result: Achieved a 24.3% reduction in tumor weight and 25.0% reduction in tumor volume at 1.25 mg/kg.
Achieved a 64.6% reduction in tumor weight and 62.5% reduction in tumor volume at 2.5 mg/kg.
Achieved an 85.1% reduction in tumor weight and 89.6% reduction in tumor volume at 5 mg/kg.
Showed no significant changes in body weight across treatment groups.
Exhibited no histopathological abnormalities in major organs compared to vehicle controls.
Demonstrated dose-dependent reduction in Ki67 expression, increased TUNEL positivity, and increased cleaved caspase-3 staining in tumor sections.
Molecular Weight

819.89

Formula

C50H60BrO3P
CAS No.
SMILES

C[C@]12[C@@]3([H])[C@@]4(CC[C@]1([H])[C@@](C)(CCC2)C(OCC5=CC=CC=C5)=O)C[C@](C(C4)=C)(CC3)OCCCCC[P+](C6=CC=CC=C6)(C7=CC=CC=C7)C8=CC=CC=C8.[Br-]
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Purity & Documentation
References
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TrxR2-IN-1 Related Classifications

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Keywords:

TrxR2-IN-13085154-16-8TrxRReactive Oxygen Species (ROS)ApoptosisCaspaseThioredoxin ReductaseASK1HeLaTrxR2MDA-MB-231hepatocellular carcinomathioredoxin reductase 2mitochondriaA549Huh7HCT116Inhibitorinhibitorinhibit

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