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^[1].

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.

TrxR1-IN-3 (5-20 mg/kg; i.p.; every other day) dose-dependently inhibits breast cancer xenograft growth in BALB/c nude mice, with the 20 mg/kg dose achieving the greatest tumor weight reduction and no detectable systemic toxicity^[1].

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

608.81

C₃₆H₅₂N₂O₆

3028398-90-2

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

• [1]. Liu Z, et al. Discovery of a novel cinnamoyl piperazinyl alepterolic acid hybrid as a TrxR1 inhibitor for inducing ROS/ER stress-mediated apoptosis in breast cancer. European journal of medicinal chemistry. 2026 Jun 06;316:119045.  [Content Brief]