Identification | Back Directory | [Name]
PR-619 | [CAS]
2645-32-1 | [Synonyms]
PR-619 CS-1128 6-Diamino-3 PR-619;PR619 PR-619, >=98% PR-619 USP/EP/BP 5-dithiocyanopyridine 2,6-DiaMino-3,5-dithiocyanopyridine 3,5-dithiocyanatopyridine-2,6-diaMine 3,5-Bis-thiocyanato-pyridine-2,6-diamine 2,6-Diaminopyridine-3,5-bis(thiocyanate) 2,6-Diamino-3,5-dithiocyanato-pyridin, 98% 2;6-DIAMINO-3;5-DITHIOCYANOPYRIDINE;PR 619;PR619 2,6-Diamino-3,5-dithiocyanopyridine PR 619 Thiocyanic acid, C,C'-(2,6-diamino-3,5-pyridinediyl) ester PR 619 2,6-Diamino-3,5-dithiocyanopyridine | [EINECS(EC#)]
200-256-5 | [Molecular Formula]
C7H5N5S2 | [MDL Number]
MFCD00830384 | [MOL File]
2645-32-1.mol | [Molecular Weight]
223.278 |
Chemical Properties | Back Directory | [Melting point ]
210℃ | [Boiling point ]
406.0±45.0 °C(Predicted) | [density ]
1.61±0.1 g/cm3(Predicted) | [storage temp. ]
?20°C | [solubility ]
DMSO: soluble5mg/mL (clear solution) | [form ]
powder | [pka]
-0.19±0.50(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Hazard Information | Back Directory | [Description]
PR-619 (2645-32-1) is a nonselective, reversible inhibitor of cysteine-reactive deubiquitinating enzymes (DUBs; 5-20 μM)1. PR-619 is highly useful for preserving ubiquitinated proteins during cell lysis. DUBs become unregulated in cell lysates and will act quickly to deubiquitinate proteins of interest during cell lysis. To preserve maximum amounts of ubiquitinated protein, include PR-619 (50-100 μM) in lysis buffers. PR-619 is also useful for interrogating the role of DUBs in intact cell systems2, and treatment of cells results in an overall accumulation of ubiquitinated proteins and many other phenotypes. | [Uses]
PR 619 is a broad-range DUB inhibitor. A selective and general inhibitior of cellular DUB activity without direct impairment of proteasomal proteolysis. Used in the preparation of thiazolopyridines an
d bisthiazolopyridines. | [Biochem/physiol Actions]
PR-619 is a cell permeable broad spectrum deubiquitylating enzymes (DBUs) inhibitor. PR-619 induces the accumulation of polyubiquitylated proteins in cells without directly affecting proteasome activity. | [Enzyme inhibitor]
This non-selective, cell-permeable pyridinamine (FW = 223.28 g/mol; CAS
2645-32-1) reversibly inhibits deubiquitinylating enzymes, or DUBs, with
EC50 values typically in the 1 to 20 μM range. Targets: ATXN3, BRCA1
Associated Protein-1 (or BAP1), Josephin domain containing-2 (or
JOSD2), Ovarian Tumor Domain-containing-5 (or OTUD5), Ubiquitin
Carboxyl-Terminal Hydrolase Isozyme-1 (or UCH-L1, UCH-L3, UCH-L5,
UCH37, Ubiquitin-Specific Peptidase-1 (or USP-1), USP-2, USP-4, USP-5,
USP-7, USP-8, USP-9X, USP-10, USP-14, USP15, USP-16, USP-19, USP-
20, USP-22, USP-24, USP-28, USP-47, USP-48, Valosin-containing protein
(or VCIP135), YOD1, as well as deISGylase PLpro, deNEDDylase DEN1,
and deSUMOlyase SENP6. | [storage]
Store at -20°C | [References]
1) Altun?et al. (2011),?Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes; Chem. Biol.,?18?1401
2) Seiberlich?et al. (2012),?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; Biochim. Biophys. Acta,?1823?2057 |
|
|