- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: PR-619
- Price: ￥518.0/10mg ￥2088.0/50mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: PR-619
- Price: $250.0/100mg $500.0/250mg $1000.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
2645-32-1
2645-32-1 structure
- Name: PR-619
- Chemical Name: (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate
- CAS Number: 2645-32-1
- Molecular Formula: C7H5N5S2
- Molecular Weight: 223.278
- Catalog: Biochemical Inhibitor Ubiquitin inhibitor DUB inhibitor
- Create Date: 2018-08-09 23:16:09
- Modify Date: 2024-01-02 12:16:48
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PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
| Name | (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate |
|---|---|
| Synonyms |
Thiocyanic acid, 2,6-diamino-3,5-pyridinediyl ester
2,6-Diaminopyridine-3,5-bis(thiocyanate) 2,6-diamino-5-(cyanothio)pyridin-3-yl thiocyanate Thiocyanic acid,2,6-diamino-3,5-pyridinediyl ester 3,5-bis-thiocyanato-pyridine-2,6-diamine HMS1440E01 2,6-Diamino-3,5-dithiocyanato-pyridin 2,6-diamino-3,5-bis(thiocyanato)pyridine QC-8206 2,6-Diamino-3,5-pyridinediyl bis(thiocyanate) 3,5-dithiocyanatopyridine-2,6-diamine PR-619 |
| Description | PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. |
|---|---|
| Related Catalog | |
| Target |
EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1] |
| In Vitro | PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation. In PR-619 treated cells, channel degradation is significantly inhibited with 87±1% of KCa3.1 still remaining after 24 hrs (n=3; P<0.05)[2]. Cell viability is determined by MTT assay and revealed that PR-619 exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM[3]. |
| Kinase Assay | Recombinant enzymes in 20 mM Tris-HCl, pH 8.0, 2 mM CaCl2 and 2 mM β-mercaptoethanol (DUB assay buffer) are preincubated with single doses or dose ranges of PR-619 or P22077 for 30 minutes in a 96 well plate before the addition of Ub-PLA2 and NBD C6-HPC. The liberation of a fluorescent product within the linear range of the assay is monitored at room temperature using a Perkin Elmer Envision fluorescence plate reader. Vehicle (2%(v/v) DMSO) and 10mM N-ethylmaleimide are included as controls. Where ≥60% inhibition is observed, EC50 values are determined using a sigmoidal dose response equation. A similar assay protocol is used to measure other in vitro enzyme assay activities[1]. |
| Cell Assay | Growth inhibition is determined with the exception that HCT-116 or HEK293T cells maintained in DMEM supplemented with 10% (v/v) FBS, 1% (v/v) penicillin/streptomycin and 2 mM L-glutamine are exposed to dose ranges of PR-619 (1, 5, 10, 20, and 50 μM) or P22077 for 72 hours[1]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 406.0±45.0 °C at 760 mmHg |
| Melting Point | 210℃ |
| Molecular Formula | C7H5N5S2 |
| Molecular Weight | 223.278 |
| Flash Point | 199.3±28.7 °C |
| Exact Mass | 222.998642 |
| PSA | 163.84000 |
| LogP | 2.05 |
| Appearance | white to beige |
| Vapour Pressure | 0.0±0.9 mmHg at 25°C |
| Index of Refraction | 1.764 |
| Storage condition | ?20°C |
| Water Solubility | DMSO: soluble5mg/mL (clear solution) |
| Symbol |
GHS05, GHS07 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H302-H315-H317-H318-H335 |
| Precautionary Statements | P261-P280-P305 + P351 + P338 |
| Hazard Codes | Xn |
| Risk Phrases | 22-37/38-41-43 |
| Safety Phrases | 26-36/37/39 |
| RIDADR | NONH for all modes of transport |
| Precursor 0 | |
|---|---|
| DownStream 1 | |
