PX-12

Catalog No.S7947 Batch:S794701

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Technical Data

Formula

C7H12N2S2
Molecular Weight 188.31 CAS No. 141400-58-0
Solubility (25°C)* In vitro DMSO 38 mg/mL (201.79 mM)
Ethanol 38 mg/mL (201.79 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
Targets
Trx-1 [1]
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 2.9μM, 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]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    MCF-7 and HT-29 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    72 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Mice bearing MCF-7 tumor xenografts

  • Dosages

    12 mg/kg

  • Administration

    i.p.

Selleck's PX-12 has been cited by 12 publications

Nuclear translocation of thioredoxin-1 promotes colorectal cancer development via modulation of the IL-6/STAT3 signaling axis through interaction with STAT3 [ Theranostics, 2023, 13(14):4730-4744] PubMed: 37771783
Nuclear translocation of thioredoxin-1 promotes colorectal cancer development via modulation of the IL-6/STAT3 signaling axis through interaction with STAT3 [ Theranostics, 2023, 13(14):4730-4744] PubMed: 37771783
The cold-inducible RNA-binding protein-Thioredoxin 1 pathway ameliorates mitochondrial dysfunction and mitochondrial dynamin-related protein 1 level in the hippocampus of aged mice with perioperative neurocognitive dysfunction [ CNS Neurosci Ther, 2023, 10.1111/cns.14433] PubMed: 37641878
Ferroptosis heterogeneity in triple-negative breast cancer reveals an innovative immunotherapy combination strategy [ Cell Metab, 2022, S1550-4131-2200411-9] PubMed: 36257316
TXN inhibitor impedes radioresistance of colorectal cancer cells with decreased ALDH1L2 expression via TXN/NF-κB signaling pathway [ Br J Cancer, 2022, 10.1038/s41416-022-01835-1] PubMed: 35597868
Thioredoxin-1 inhibits amyloid-β25-35-induced activation of NLRP1/caspase-1/GSDMD pyroptotic pathway in PC12 cells [ Mol Biol Rep, 2022, 10.1007/s11033-022-07177-8] PubMed: 35072836
Thioredoxin activity confers resistance against oxidative stress in tumor-infiltrating NK cells [ J Clin Invest, 2020, 137585] PubMed: 32673292
Up-regulation of thioredoxin system by puerarin inhibits lipid uptake in macrophages [ Free Radic Biol Med, 2020, S0891-5849(20)31609-9] PubMed: 33242606
Bakuchiol Attenuates Oxidative Stress and Neuron Damage by Regulating Trx1/TXNIP and the Phosphorylation of AMPK After Subarachnoid Hemorrhage in Mice [ Front Pharmacol, 2020, 15;11:712] PubMed: 32499702
Adiponectin Peptide Alleviates Oxidative Stress and NLRP3 Inflammasome Activation After Cerebral Ischemia-Reperfusion Injury by Regulating AMPK/GSK-3β [ Exp Neurol, 2020, 329:113302] PubMed: 32275928

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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