TrxR1-IN-3
TrxR1-IN-3 is a selective TrxR1 inhibitor with an IC50 of 1.19 μM. TrxR1-IN-3 increases intracellular reactive oxygen species (ROS) levels, induces endoplasmic reticulum (ER) stress, and activates Caspase-dependent Apoptosis. TrxR1-IN-3 exhibits anticancer activity against multiple breast cancer subtypes, including triple-negative breast cancer (TNBC). TrxR1-IN-3 can be used in breast cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 3028398-90-2
- Formula: C36H52N2O6
- Molecular Weight:608.81
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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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TrxR1 1.19 μM (IC50) |
TrxR1-IN-3 (Compound 6M) (Gradient concentrations; 72 h) potently inhibits the proliferation of MCF7, MDA-MB-231, MDA-MB-468, and BT474 breast cancer cells with IC50 values ranging from 0.94 μM to 2.53 μM, and exhibits low cytotoxicity toward normal MCF-10A breast epithelial cells with a selectivity index exceeding 10 for all tested cancer cell lines[1].
TrxR1-IN-3 (Gradient concentrations; 2 h) potently inhibits purified rat TrxR1 activity with an IC50 of 1.19 μM, primarily targeting the Sec-498 residue, as evidenced by its drastically reduced inhibitory potency (IC50 > 10 μM) against the human U498C TrxR1 mutant[1].
TrxR1-IN-3 (1-10 μM) selectively inhibits cellular TrxR activity in MCF7 cells with an IC50 of 2.99 μM, while having minimal inhibitory effects on GR and GPx even at 10 μM[1].
TrxR1-IN-3 (1-5 μM; 24 h) dose-dependently inhibits intracellular TrxR activity in MCF7 and MDA-MB-231 breast cancer cells[1].
TrxR1-IN-3 (1-5 μM; 24 h) dose-dependently reduces the clonogenic capacity of MCF7 and MDA-MB-231 breast cancer cells[1].
TrxR1-IN-3 (3-5 μM; 24 h) dose-dependently induces apoptosis in MCF7 and MDA-MB-231 breast cancer cells[1].
TrxR1-IN-3 (3-5 μM) induces caspase-dependent apoptosis in MCF7 and MDA-MB-231 breast cancer cells via activation of both extrinsic and intrinsic pathways, as evidenced by cleavage of caspase-8, caspase-9, and PARP, with this effect blocked by pre-incubation with the pan-caspase inhibitor Z-VAD[1].
TrxR1-IN-3 (1-5 μM; 24 h) dose-dependently elevates intracellular ROS levels in MCF7 and MDA-MB-231 breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 3-4 weeks old, subcutaneous xenograft model)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; every other day
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Result:Significantly inhibited tumor growth compared to the control group.
Reduced mean tumor weight to ~140 mg (5 mg/kg), ~80 mg (10 mg/kg), and ~30 mg (20 mg/kg), relative to ~240 mg in the control group.
Dose-dependently reduced relative tumor proliferation rates (T/C) over the 30-day treatment period.
Caused no obvious body weight loss in any treatment group, indicating no systemic toxicity at the administered doses.
Chemical Information
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CAS No. 3028398-90-2
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Molecular Weight 608.81
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Formula C36H52N2O6
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SMILES
COC1=CC(/C=C/C(N2CCN(C(/C=C(C)/CC[C@@]3([H])[C@@](CC[C@@H](O)C4(C)C)(C)[C@]4([H])CCC3=C)=O)CC2)=O)=CC(OC)=C1OC
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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)