PR-619（Cat No.:I002906）is a potent and selective inhibitor of deubiquitinating enzymes (DUBs), playing a crucial role in the regulation of protein degradation and signaling pathways. By inhibiting DUB activity, PR-619 disrupts the removal of ubiquitin from target proteins, leading to altered cellular processes, including apoptosis and cell cycle regulation. This compound has shown potential in preclinical studies for enhancing the efficacy of cancer therapies and in treating neurodegenerative diseases by modulating protein homeostasis. Ongoing research is focused on its therapeutic applications and the exploration of its mechanism in various disease models.
| Catalog Number | I002906 |
| CAS Number | 2645-32-1 |
| Synonyms | (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate |
| Molecular Formula | C₇H₅N₅S₂ |
| Purity | ≥95% |
| Target | DUB |
| Solubility | DMSO: ≥ 21 mg/mL |
| Storage | Store at -20°C |
| IC50 | 3.93 μM (EC50, USP4); 7.2 μM (EC50, USP2 core); 5.10 μM (EC50, USP20) [1] |
| IUPAC Name | (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate |
| InChI | InChI=1S/C7H5N5S2/c8-2-13-4-1-5(14-3-9)7(11)12-6(4)10/h1H,(H4,10,11,12) |
| InChIKey | ZXOBLNBVNROVLC-UHFFFAOYSA-N |
| SMILES | C1=C(C(=NC(=C1SC#N)N)N)SC#N |
| Reference | </br>1:The Deubiquitinase Inhibitor PR-619 Sensitizes Normal Human Fibroblasts to Tumor Necrosis Factor-related Apoptosis-inducing Ligand (TRAIL)-mediated Cell Death. Crowder RN, Dicker DT, El-Deiry WS.J Biol Chem. 2016 Mar 11;291(11):5960-70. doi: 10.1074/jbc.M115.713545. Epub 2016 Jan 12. PMID: 26757822 Free PMC Article</br>2:Inhibition of protein deubiquitination by PR-619 activates the autophagic pathway in OLN-t40 oligodendroglial cells. Seiberlich V, Borchert J, Zhukareva V, Richter-Landsberg C.Cell Biochem Biophys. 2013 Sep;67(1):149-60. doi: 10.1007/s12013-013-9622-8. PMID: 23686611 </br>3:The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases. Seiberlich V, Goldbaum O, Zhukareva V, Richter-Landsberg C.Biochim Biophys Acta. 2012 Nov;1823(11):2057-68. doi: 10.1016/j.bbamcr.2012.04.011. Epub 2012 Apr 28. PMID: 22565157 Free Article |
