TrxR-IN-6

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TrxR-IN-6 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-6 induces reactive oxygen species (ROS) accumulation and cell apoptosis. TrxR-IN-6 induces mitochondrial dysfunction, endoplasmic reticulum stress and DNA damage. TrxR-IN-6 can be used for the research of breast cancer, leukemia.

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

TrxR-IN-6 Chemical Structure

CAS No. : 3032446-53-7

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TrxR1 TrxR2

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.98 μM Compound: 1b	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]
COS-7	IC₅₀	3.74 μM Compound: 1b	Antiproliferative activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]
HeLa	IC₅₀	0.69 μM Compound: 1b	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]
MCF7	IC₅₀	1.79 μM Compound: 1b	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]
MOLM-13	IC₅₀	0.91 μM Compound: 1b	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]
NB-4	IC₅₀	0.96 μM Compound: 1b	Antiproliferative activity against human NB4 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human NB4 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37688544]

In Vitro

TrxR-IN-6 (Compound 1d) (24-48 h) potently inhibits proliferation of 4T1, MCF-7, HeLa, Molm-13, and K562 cancer cells with IC₅₀ values ranging from 0.45 μM to 0.74 μM, while exhibiting low toxicity to COS-7 normal cells and PBMC^[1].
TrxR-IN-6 (0.5-2 μM; 12-24 h) selectively inhibits TrxR activity in 4T1 and MCF-7 cancer cells in vitro in a concentration-dependent manner, with no effect on TrxR activity in COS-7 normal cells or on GR/GPx activity in 4T1 cells^[1].
TrxR-IN-6 (0.5-2 μM; 24 h) reduces TrxR system mRNA and protein levels in 4T1 and MCF-7 cancer cells, but not in COS-7 normal cells, and its anti-proliferative and pro-apoptotic effects are dependent on TrxR expression in 4T1 cells^[1].
TrxR-IN-6 (0.5-2 μM; 3-24 h) induces irreversible oxidative stress in 4T1 cells^[1].
TrxR-IN-6 (0.5-2 μM; 12-24 h) triggers endoplasmic reticulum stress and unfolded protein response in 4T1 cells by upregulating ER stress-related proteins and disrupting cytoplasmic calcium homeostasis^[1].
TrxR-IN-6 (0.5-2 μM; 12-24 h) induces mitochondrial dysfunction in 4T1 cells by reducing membrane potential and ATP levels, altering Bcl-2 family protein expression, activating the caspase apoptotic cascade, inducing DNA fragmentation, and causing structural mitochondrial damage^[1].
TrxR-IN-6 (1-2 μM; 24 h) induces caspase-dependent apoptosis in 4T1 cells in vitro in a concentration-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	4T1
Concentration:	0.5 μM; 1 μM; 2 μM
Incubation Time:	24 h
Result:	Upregulated the levels of relevant proteins involved in ER stress, including GRP78, PERK, ATF4, and CHOP. Strongly upregulated ubiquitinated protein levels.

Western Blot Analysis^[1]

Cell Line:	4T1
Concentration:	0.5 μM; 1 μM; 2 μM
Incubation Time:	24 h
Result:	Upregulated the expression of Bax, c-casp9, c-casp-3 and c-parp. Downregulated the expression of Bcl-2.

Apoptosis Analysis^[1]

Cell Line:	4T1
Concentration:	0.5 μM; 1 μM; 2 μM
Incubation Time:	24 h
Result:	Induced apoptosis in a concentration-dependent manner, with 21.8% early apoptosis and 29.9% late apoptosis/necrosis at 2 μM.

In Vivo

TrxR-IN-6 (Compound 1d) (1.5 mg/kg; i.p.; once weekly; 2 weeks) induces 90% tumor shrinkage in BALB/c mice with 4T1 breast cancer xenografts^[1].

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

Animal Model:	BALB/c (female, 4-week-old, 18-22 g, subcutaneous injection of 2 × 10⁶ 4T1 cells)^[1]
Dosage:	1.5 mg/kg
Administration:	i.p.; once weekly; 2 weeks
Result:	Induced 90% tumor shrinkage, resulting in significantly smaller tumor volumes and lower tumor weights compared to control and auranofin-treated groups. Reduced protein levels of TrxR1, Trx1, TrxR2, and Trx2 in tumor tissue. Triggered a robust ROS burst in tumors. Did not cause significant changes in mouse body weight. Reversed spleen enlargement observed in control tumor-bearing mice. Protected liver cells from tumor-related damage with no obvious abnormalities in other organs. Normalized hematological parameters including white blood cells, neutrophils, lymphocytes, and monocytes compared to control tumor-bearing mice.

Molecular Weight

384.18

Formula

C₁₁H₁₂AsCl₂NOS₂

CAS No.

3032446-53-7

SMILES

O=C(NC1=CC=C([As]2SCCCS2)C=C1)C(Cl)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. She W, et al. Discovery of novel organoarsenicals as robust thioredoxin reductase inhibitors for oxidative stress mediated cancer therapy. Biochem Pharmacol. 2023;218:115908. [Content Brief]

TrxR-IN-6 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-63032446-53-7TrxRApoptosisReactive Oxygen Species (ROS)Thioredoxin Reductase4T1PBMCleukemiathioredoxin reductaseMCF-7Molm-13K562HeLaCOS-7breast cancerInhibitorinhibitorinhibit

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