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PX-12

Catalog No. T2283 CAS 141400-58-0

Synonyms: IV-2, PX12

PX-12 (PX12) (1-methylpropyl 2-imidazolyl disulfide) is a small-molecule inhibitor of Trx-1 (thioredoxin-1), stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, PX-12 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of Px-12 with increased patient survival.

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PX-12, CAS 141400-58-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 133.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 413.00
500 mg	In stock	$ 943.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.6%

Purity: 99%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	PX-12 (PX12) (1-methylpropyl 2-imidazolyl disulfide) is a small-molecule inhibitor of Trx-1 (thioredoxin-1), stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, PX-12 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of Px-12 with increased patient survival.
Targets&IC50	MCF-7 cells:1.9 μM, HT29 cells:2.9 μM
In vitro	In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9 μM, respectively. [1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. [2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. [3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. [4]
In vivo	In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. [1]
Cell Research	Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.(Only for Reference)

Synonyms	IV-2, PX12
Molecular Weight	188.31
Formula	C7H12N2S2
CAS No.	141400-58-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 38 mg/mL (201.79 mM)

DMSO: 18.8 mg/mL(100 mM)

References and Literature

1. Welsh SJ, et al. Mol Cancer Ther. 2003, 2(3), 235-243. 2. Kim YH, et al. Cancer Chemother Pharmacol. 2011, 68(2), 405-413. 3. You BR, et al. Int J Oncol. 2014, 44(1), 301-308. 4. Li GZ, et al. Am J Transl Res. 2015, 7(9), 1528-1540. 6. Metcalfe C, et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation. PLoS One. 2016 Oct 7;11(10):e0163006

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Bioactive Compounds Library Max Ferroptosis Compound Library Covalent Inhibitor Library Metabolism Compound Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PX-12 141400-58-0 Metabolism Thioredoxin IV 2 inhibit IV-2 Inhibitor IV2 PX 12 PX12 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.