PX-12
Based on 13 publication(s) in Google Scholar
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 141400-58-0
- Formula: C7H12N2S2
- Molecular Weight:188.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) PX-12
More- Cell Host Microbe. 2025 Sep 30:S1931-3128(25)00375-0. [Abstract]
- Nat Commun. 2025 Sep 2;16(1):8181. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Int J Nanomedicine. 2024 Dec 31:19:14125-14141. [Abstract]
- Free Radic Biol Med. 2024 Jun:218:132-148. [Abstract]
- Free Radic Biol Med. 2022 Jul 31;189:157-168. [Abstract]
- Free Radic Biol Med. 2022 Jan:178:246-261. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Front Immunol. 2021 Mar 9:12:625957. [Abstract]
- Ecotoxicol Environ Saf. 2022 Dec 1:247:114263. [Abstract]
- J Biol Chem. 2017 Jun 2;292(22):9136-9149. [Abstract]
- Cytotechnology. 2026 Jun;78(3):116. [Abstract]
- Patent. US20250161243A1.
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Cell Proliferation/Viability Assay
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IF
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Histological Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
Biological Activity
IC50: 1.9 (MCF-7), 2.9 μM (HT-29 cells)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>20 μM
Compound: PX-12
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 36657375] |
| HeLa | IC50 |
9 μM
Compound: PX-12
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 36657375] |
| HepG2 | IC50 |
12 μM
Compound: PX-12
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 36657375] |
| HT-29 | GI50 |
25 μM
Compound: PX-12
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Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method
Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method
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[PMID: 18617414] |
| HT-29 | GI50 |
25 μM
Compound: PX-12
|
Antiproliferative activity against human HT29 cells
Antiproliferative activity against human HT29 cells
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[PMID: 18502639] |
| M21 | GI50 |
8.3 μM
Compound: PX-12
|
Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method
Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method
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[PMID: 18617414] |
| M21 | GI50 |
8.3 μM
Compound: PX-12
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Antiproliferative activity against human M21 cells
Antiproliferative activity against human M21 cells
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[PMID: 18502639] |
| MCF7 | GI50 |
8.3 μM
Compound: PX-12
|
Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method
Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method
|
[PMID: 18617414] |
| MCF7 | GI50 |
8.3 μM
Compound: PX-12
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
|
[PMID: 18502639] |
| T84 | IC50 |
2.11 μM
Compound: 1, PX-12
|
Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis
Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis
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[PMID: 23327656] |
| Vero C1008 | IC50 |
0.67 μM
Compound: 14; PX-12
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Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
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[PMID: 37244162] |
PX-12 inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively[1].
PX-12 particularly reduces the activity of Trx-1 by means of thio-alkylating critical cysteine residue (Cys73) which is located in the outside the conserved redox catalytic site of Trx-1. PX-12 affects the oxidation state of thiols in a number of cell surface proteins. Key surface receptors for platelet adhesion and activation are affected, including the collagen receptor GPVI and the von Willebrand factor receptor, GPIb. PX-12 inhibits thrombus formation over Type I collagen in whole blood under flow conditions[2].
Thioredoxin-1 (Trx-1) is a cellular redox protein that promotes tumor growth, inhibits apoptosis, and up-regulates hypoxia-inducible factor-1α and vascular endothelial growth factor[3].
PX-12 inhibits the growth of colorectal cancer DLD-1 and SW620 cells in a dose- and time-dependent manner. PX-12 reduces cell colony formation and induced a G2/M phase arrest of the cell cycle. PX-12 treatment induces apoptosis. PX-12 inhibits colorectal cancer cell migration and invasion. Treatment of cancer cells with PX-12 reduces NOX1, CDH17 and S100A4 mRNA expression, and increases KLF17 mRNA expression. PX-12 decreases S100A4 protein expression in the colorectal cancer cells[4].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 141400-58-0
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Appearance Solid
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Molecular Weight 188.31
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Formula C7H12N2S2
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Color White to light yellow
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SMILES
CC(CC)SSC1=NC=CN1
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Synonyms
IV-2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
Immunometabolic reprogramming of macrophages by gut microbiota-derived cadaverine controls colon inflammation. [Abstract]2025 Sep 30:S1931-3128(25)00375-0. PMID: 41033313 -
Nat Commun
Targeting ALDH16A1 mediated thioredoxin lysosomal degradation to enhance ferroptosis susceptibility in SMARCA4-deficient NSCLC. [Abstract]2025 Sep 2;16(1):8181. PMID: 40897711
PX-12 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 2;16(1):8181. [Abstract]
Cell viability in PC9 and A549 cells treated with 10 μM auranofin, PX-12, or conoidin A combined with or without DFO (100 μM) or Fer-1 (10 μM) for 24 h.
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Int J Nanomedicine
Nano Acacetin Mitigates Intestinal Mucosal Injury in Sepsis Rats by Protecting Mitochondrial Function and Regulating TRX1 to Inhibit the NLRP3 Pyroptosis Pathway. [Abstract]2024 Dec 31:19:14125-14141. PMID: 39759963 -
Free Radic Biol Med
Hydrogen alleviates impaired lung epithelial barrier in acute respiratory distress syndrome via inhibiting Drp1-mediated mitochondrial fission through the Trx1 pathway. [Abstract]2024 Jun:218:132-148. PMID: 38554812
PX-12 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Jun:218:132-148. [Abstract]
The BEAS-2B cells were pre-treated with DMSO or LPS (1 μg/ml) and then exposed to hydrogen (60%) with or without PX-12 (8 μM) for another 12 h (n = 3). Representative immunofluorescence images of staining for Trx1 (red), COXIV (green), and DAPI (blue) in BEAS-2B cells in different groups (n = 3) were shown. The results showed that adding PX-12 inhibited Trx1 expression. Scale bars, 10 μm.
PX-12 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Jun:218:132-148. [Abstract]
Mice were pre-treated with saline or LPS (10 mg/kg; i.p.) before inhalation of air or hydrogen (4%; i.p.) with or without PX-12 (12 mg/kg; i.p.) for another 12 h. Hematoxylin and eosin staining was used to evaluate the lung histopathology (n = 5). The results showed that PX-12 reversed the protective effect of hydrogen against LPS-induced pulmonary inflammation by inhibiting Trx1, indicating that the protective action of hydrogen was related to the Trx1 pathway.
PX-12 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Jun:218:132-148. [Abstract]
Mice were pre-treated with saline or LPS (10 mg/kg; i.p.) before inhalation of air or hydrogen (4%; i.p.) with or without PX-12 (12 mg/kg; i.p.) for another 12 h. Protein blots of occludin, ZO-1 and cleaved caspase-3 were detected by Western blot (n = 3). The results showed that PX-12 reversed the ameliorative effect of hydrogen on LPS-induced epithelial barrier damage in mice by inhibiting Trx1.
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Free Radic Biol Med
Diallyl trisulfide sensitizes radiation therapy on glioblastoma through directly targeting thioredoxin 1. [Abstract]2022 Jul 31;189:157-168. PMID: 35921994 -
Free Radic Biol Med
Inhibition of Nrf2 degradation alleviates age-related osteoporosis induced by 1,25-Dihydroxyvitamin D deficiency. [Abstract]2022 Jan:178:246-261. PMID: 34890768 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Front Immunol
Hydrogen Attenuates Endotoxin-Induced Lung Injury by Activating Thioredoxin 1 and Decreasing Tissue Factor Expression. [Abstract]2021 Mar 9:12:625957. PMID: 33767697 -
Ecotoxicol Environ Saf
Low-dose arsenite causes overexpression of EGF, TGFα, and HSP90 through Trx1-TXNIP-NLRP3 axis mediated signaling pathways in the human bladder epithelial cells. [Abstract]2022 Dec 1:247:114263. PMID: 36343453 -
J Biol Chem
Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. [Abstract]2017 Jun 2;292(22):9136-9149. PMID: 28411237
PX-12 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2017 Jun 2;292(22):9136-9149. [Abstract]
The plate clone formation of SW480 and SW620 cells with Gemcitabine (8 nM in SW480 and 16 nM in SW620) and/or PX-12 (4 μM in SW480 and 8 μM in SW620).
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Cytotechnology
PX-12 exhibits cytotoxic and anti-migration effects in colorectal cancer cells under Hypoxia-like conditions induced by Dimethyloxalylglycine. [Abstract]2026 Jun;78(3):116. PMID: 42145842 -
Solvent & Solubility
Ethanol : 50 mg/mL (265.52 mM; Need ultrasonic)
DMSO : ≥ 44.7 mg/mL (237.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (13.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Welsh SJ, et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol Cancer Ther. 2003 Mar;2(3):235-43. [Content Brief]
[2]. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149. [Content Brief]
[3]. Metcalfe C, et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation. PLoS One. 2016 Oct 7;11(10):e0163006 [Content Brief]
[4]. Ramanathan RK, et al. A Phase I pharmacokinetic and pharmacodynamic study of PX-12, a novel inhibitor of thioredoxin-1, in patients with advanced solid tumors. Clin Cancer Res. 2007 Apr 1;13(7):2109-14. [Content Brief]
[5]. Wang F, et al. Thioredoxin-1 inhibitor, 1-methylpropyl 2-imidazolyl disulfide, inhibits the growth, migration and invasion of colorectal cancer cell lines. Oncol Rep. 2015 Feb;33(2):967-73. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 5.3104 mL | 26.5520 mL | 53.1039 mL | 132.7598 mL |
| 5 mM | 1.0621 mL | 5.3104 mL | 10.6208 mL | 26.5520 mL | |
| 10 mM | 0.5310 mL | 2.6552 mL | 5.3104 mL | 13.2760 mL | |
| 15 mM | 0.3540 mL | 1.7701 mL | 3.5403 mL | 8.8507 mL | |
| 20 mM | 0.2655 mL | 1.3276 mL | 2.6552 mL | 6.6380 mL | |
| 25 mM | 0.2124 mL | 1.0621 mL | 2.1242 mL | 5.3104 mL | |
| 30 mM | 0.1770 mL | 0.8851 mL | 1.7701 mL | 4.4253 mL | |
| 40 mM | 0.1328 mL | 0.6638 mL | 1.3276 mL | 3.3190 mL | |
| 50 mM | 0.1062 mL | 0.5310 mL | 1.0621 mL | 2.6552 mL | |
| 60 mM | 0.0885 mL | 0.4425 mL | 0.8851 mL | 2.2127 mL | |
| 80 mM | 0.0664 mL | 0.3319 mL | 0.6638 mL | 1.6595 mL | |
| 100 mM | 0.0531 mL | 0.2655 mL | 0.5310 mL | 1.3276 mL |