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PX-12 [141400-58-0]

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Referencia HY-13734-1mL

embalaje : 10mM/1mL

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Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Contact local distributor :

Teléfono : +1 850 650 7790

Descripciòn

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]
HT-29	GI₅₀	25 μM Compound: PX-12	Antiproliferative activity against human HT29 cells Antiproliferative activity against human HT29 cells	[PMID: 18502639]
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]
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]
M21	GI₅₀	8.3 μM Compound: PX-12	Antiproliferative activity against human M21 cells Antiproliferative activity against human M21 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]
MCF7	GI₅₀	8.3 μM Compound: PX-12	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 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]
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.

Solvente y solubilidad

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 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 DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

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.
Protocol 4

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.
Protocol 5

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.

Pureza y Documentación

Purity: 99.96%

Ficha de datos (277 KB) SDS (393 KB)

COA (246 KB) HNMR (234 KB) RP-HPLC (258 KB) MS (103 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

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PX-12 [141400-58-0]

Referencia HY-13734-1mL

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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