PX-12

CHF 30.00
In stock
AG-CR1-3739-M0011 mgCHF 30.00
AG-CR1-3739-M0055 mgCHF 70.00
AG-CR1-3739-M02525 mgCHF 210.00
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Product Details
Synonyms IV-2; 2-[(1-Methylpropyl)dithio]-1H-imidazole
Product Type Chemical
Properties
Formula

C7H12N2S2

MW 188.3
CAS 141400-58-0
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white powder.
Solubility Soluble in DMSO, ethanol or DMF (all 15mg/ml). Slightly soluble in water (~1mg/ml).
Identity Determined by 1H-NMR.
InChi Key BPBPYQWMFCTCNG-UHFFFAOYSA-N
Smiles CC(CC)SSC1=NC=CN1
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • PX-12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme.
  • High levels of Trx-1 have been associated with colorectal, gastric and lung cancers. PX-12 stimulates apoptosis, down-regulates HIF-1α, vascular endothelial growth factor (VEGF) and iNOS, and consequently inhibits proliferation and tumor growth in animal models. It has also been reported to inhibit tubulin polymerization in vitro, induce cell cycle arrest at G2/M phase and inhibit growth, migration and invasion of several cancer cell lines.
  • PX-12 shows antiviral activity against HIV-1, by inhibiting the enzymatic activity of Trx1 and the Trx1-dependent disulfide reduction of gp120. Microtubule polymerization and formation of acetylated microtubules are inhibited as well, activities shown to be required for HIV-1 life cycle propagation.
  • PX-12 has broad spectrum antimicrobial activity targeting the thioredoxin system of bacterial, fungal, protozoan and helminth pathogens without significant toxicity to the host.
  • PX-12 potentially inhibits the 33.8-kDa Main protease (Mpro)/3C-like protease of SARS-CoV-2, consequently inhibiting viral transcription and replication and possibly inhibiting spread of COVID-19.
Product References
  1. Reversible inhibition of human thioredoxin reductase activity by cytotoxic alkyl 2-imidazolyl disulfide analogues: J.E. Oblong, et al.; Cancer Chemother. Pharmacol. 34, 434 (1994)
  2. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation: S.J. Welsh, et al.; Mol. Cancer Ther. 2, 235 (2003)
  3. The antitumor thioredoxin-1 inhibitor PX-12 (1-methylpropyl 2-imidazolyl disulfide) decreases thioredoxin-1 and VEGF levels in cancer patient plasma: A.F. Baker, et al.; J. Lab. Clin. Med. 147, 83 (2006)
  4. Drug evaluation: the thioredoxin inhibitor PX-12 in the treatment of cancer: C.M. Galmarini; Curr. Opin. Investig. Drugs 7, 1108 (2006) (Review)
  5. 2-[(1-methylpropyl)dithio]-1H-imidazole inhibits tubulin polymerization through cysteine oxidation: K. Huber, et al.; Mol. Cancer Ther. 7, 143 (2008)
  6. PX-12 inhibits the growth of A549 lung cancer cells via G2/M phase arrest and ROS-dependent apoptosis: B.R. You, et al.; Int. J. Oncol. 44, 301 (2014)
  7. PX-12 induces apoptosis in Calu-6 cells in an oxidative stress-dependent manner: B.R. You, et al.; Tumour Biol. 36, 2087 (2015)
  8. Thioredoxin-1 inhibitor, 1-methylpropyl 2-imidazolyl disulfide, inhibits the growth, migration and invasion of colorectal cancer cell lines: F. Wang, et al.; Oncol. Rep. 33, 967 (2015)
  9. Repurposing Auranofin, Ebselen, and PX-12 as Antimicrobial Agents Targeting the Thioredoxin System: H.C. May, et al.; Front. Microbiol. 9, 336 (2018)
  10. Inhibition of the thioredoxin system by PX-12 (1-methylpropyl 2-imidazolyl disulfide) impedes HIV-1 infection in TZM-bl cells: M. Lundberg, et al.; Sci. Rep. 9, 5656 (2019)
  11. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors: Z. Jin, et al.; Nature 582, 289 (2020)
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