Art. -Nr.: HY-13734

PX-12

(Synonyms: IV-2)

13 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.96%
CAS. Nr.: 141400-58-0
Formel: C₇H₁₂N₂S₂
Molecular Weight:188.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PX-12 Chemical Structure

CAS. Nr.: 141400-58-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target

IC50: 1.9 (MCF-7), 2.9 μM (HT-29 cells)^[1]

Cellular Effect

Cell Line	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	[PMID: 36657375]
HeLa	IC₅₀	9 μM Compound: PX-12	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	[PMID: 36657375]
HepG2	IC₅₀	12 μM Compound: PX-12	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	[PMID: 36657375]
HT-29	GI₅₀	25 μM Compound: PX-12	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	[PMID: 18617414]
HT-29	GI₅₀	25 μM Compound: PX-12	Antiproliferative activity against human HT29 cells Antiproliferative activity against human HT29 cells	[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	[PMID: 18617414]
M21	GI₅₀	8.3 μM Compound: PX-12	Antiproliferative activity against human M21 cells Antiproliferative activity against human M21 cells	[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	[PMID: 23327656]
Vero C1008	IC₅₀	0.67 μM Compound: 14; PX-12	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	[PMID: 37244162]

In Vitro

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.

In Vivo

PX-12 has been shown to have in vivo antitumor activity against human tumor xenografts including HT-29 colon cancer in SCID mice and has been tested in a phase I clinical trial in patients^[3].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 141400-58-0
Appearance Solid
Molecular Weight 188.31
Formel C₇H₁₂N₂S₂
Color White to light yellow
SMILES

CC(CC)SSC1=NC=CN1
Synonyms

IV-2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All IFCell Proliferation/Viability AssayHistological Imaging/StainingWB

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Journal Impact Factor

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.
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.
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).
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
Patent

US20250161243A1.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.3104 mL

26.5520 mL

53.1039 mL

5 mM

1.0621 mL

5.3104 mL

10.6208 mL

10 mM

0.5310 mL

2.6552 mL

5.3104 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)