For research use only. Not for therapeutic Use.
PX-12（Cat No.:I001577）is a potent small-molecule inhibitor of thioredoxin-1 (Trx-1), a key regulator of cellular redox balance. By inhibiting Trx-1, PX-12 disrupts the redox state of cancer cells, leading to oxidative stress and apoptosis. It has been investigated for its potential anti-tumor effects, particularly in cancers where Trx-1 is overexpressed, such as pancreatic and lung cancers. PX-12 is of great interest in cancer research due to its role in targeting the redox system, offering a novel therapeutic approach in oncology.
| Catalog Number | I001577 |
| CAS Number | 141400-58-0 |
| Synonyms | 2-(butan-2-yldisulfanyl)-1H-imidazole |
| Molecular Formula | C₇H₁₂N₂S₂ |
| Purity | ≥95% |
| Target | HIF |
| Solubility | DMSO: ≥ 47.7 mg/mL |
| Storage | Store at 4°C |
| IC50 | 7 uM (Hela,72 h, MTT) [1] |
| IUPAC Name | 2-(butan-2-yldisulfanyl)-1H-imidazole |
| InChI | InChI=1S/C7H12N2S2/c1-3-6(2)10-11-7-8-4-5-9-7/h4-6H,3H2,1-2H3,(H,8,9) |
| InChIKey | BPBPYQWMFCTCNG-UHFFFAOYSA-N |
| SMILES | CCC(C)SSC1=NC=CN1 |
| Reference | </br>1:Upregulation of connexin43 contributes to PX-12-induced oxidative cell death. Li G, Gao K, Chi Y, Zhang X, Mitsui T, Yao J, Takeda M.Tumour Biol. 2016 Jun;37(6):7535-46. doi: 10.1007/s13277-015-4620-7. Epub 2015 Dec 18. PMID: 26684802 </br>2:PX-12 inhibits the growth of hepatocelluar carcinoma by inducing S-phase arrest, ROS-dependent apoptosis and enhances 5-FU cytotoxicity. Li GZ, Liang HF, Liao B, Zhang L, Ni YA, Zhou HH, Zhang EL, Zhang BX, Chen XP.Am J Transl Res. 2015 Sep 15;7(9):1528-40. eCollection 2015. PMID: 26550453 Free PMC Article</br>3:PX-12 induces apoptosis in Calu-6 cells in an oxidative stress-dependent manner. You BR, Shin HR, Han BR, Park WH.Tumour Biol. 2015 Mar;36(3):2087-95. doi: 10.1007/s13277-014-2816-x. Epub 2014 Nov 13. PMID: 25391429 </br>4:Thioredoxin-1 inhibitor PX-12 induces human acute myeloid leukemia cell apoptosis and enhances the sensitivity of cells to arsenic trioxide. Tan Y, Bi L, Zhang P, Wang F, Lin F, Ni W, Wu J, Jiang L.Int J Clin Exp Pathol. 2014 Jul 15;7(8):4765-73. eCollection 2014. PMID: 25197347 Free PMC Article</br>5:PX-12-induced HeLa cell death is associated with oxidative stress and GSH depletion. Shin HR, You BR, Park WH.Oncol Lett. 2013 Dec;6(6):1804-1810. Epub 2013 Oct 21. PMID: 24260080 Free PMC Article</br>6:PX-12 inhibits the growth of A549 lung cancer cells via G2/M phase arrest and ROS-dependent apoptosis. You BR, Shin HR, Park WH.Int J Oncol. 2014 Jan;44(1):301-8. doi: 10.3892/ijo.2013.2152. Epub 2013 Oct 29. PMID: 24172913 </br>7:Effects of the thioredoxin-1 inhibitor PX-12 on blood-brain barrier permeability in the early stage of focal cerebral ischemia. Chi OZ, Barsoum S, Grayson J, Liu X, Weiss HR.Pharmacology. 2013;92(3-4):175-81. doi: 10.1159/000354583. Epub 2013 Sep 21. PMID: 24060905 </br>8:A phase IB trial of 24-hour intravenous PX-12, a thioredoxin-1 inhibitor, in patients with advanced gastrointestinal cancers. Baker AF, Adab KN, Raghunand N, Chow HH, Stratton SP, Squire SW, Boice M, Pestano LA, Kirkpatrick DL, Dragovich T.Invest New Drugs. 2013 Jun;31(3):631-41. doi: 10.1007/s10637-012-9846-2. Epub 2012 Jun 19. PMID: 22711542 Free PMC Article</br>9:A phase I trial of PX-12, a small-molecule inhibitor of thioredoxin-1, administered as a 72-hour infusion every 21 days in patients with advanced cancers refractory to standard therapy. Ramanathan RK, Stephenson JJ, Weiss GJ, Pestano LA, Lowe A, Hiscox A, Leos RA, Martin JC, Kirkpatrick L, Richards DA.Invest New Drugs. 2012 Aug;30(4):1591-6. doi: 10.1007/s10637-011-9739-9. Epub 2011 Aug 24. PMID: 21863237 </br>10:Antitumor agent PX-12 inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase in spermidine/spermine acetyl transferase. Kim YH, Coon A, Baker AF, Powis G.Cancer Chemother Pharmacol. 2011 Aug;68(2):405-13. doi: 10.1007/s00280-010-1500-0. Epub 2010 Nov 11. PMID: 21069338 Free PMC Article |
