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.
- CAS No.: 3085154-16-8
- Formula: C50H60BrO3P
- Molecular Weight:819.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
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TrxR2 0.83 μM () |
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.
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Cell Line:Huh7
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Concentration:0.8 μM; 1.6 μM
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Incubation Time:24 h
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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.
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Cell Line:Huh7
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Concentration:0.4 μM; 0.8 μM; 1.6 μM
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Incubation Time:24 h
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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.
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Cell Line:Huh7, HHL5
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Concentration:0.4 μM; 0.8 μM; 1.6 μM
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Incubation Time:24 h
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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.
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Cell Line:Huh7
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Concentration:0.4 μM; 0.8 μM; 1.6 μM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cA-nude (female, 5-6 weeks old, 19−21 g, subcutaneous inoculation of Huh7 cells)[1]
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Dosage:1.25 mg/kg; 2.5 mg/kg; 5 mg/kg
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Administration:subcutaneous injection; every 2 days for 14 days
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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.
Chemical Information
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CAS No. 3085154-16-8
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Molecular Weight 819.89
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Formula C50H60BrO3P
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TrxR2-IN-1 Related Classifications
HY-182324 Related Classifications
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