| 名称 | PR-619 |
| 描述 | PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a DUB inhibitor that inhibits USP2/4/5/7/8 (EC50=7.2/3.93/8.61/6.86/4.9 μM). PR-619 induces endoplasmic reticulum stress and activates autophagy. |
| 细胞实验 | 72 h hours later, 0.2 mg/mL resazurin prepared in phosphate-buffered saline is added to each well and the cells are incubated for an additional 3-6 h. The fluorescence of the resazurin reduction product is measured using Ex=535 nm and Em=590 nm filters on a fluorimeter. The EC50 values are calculated in Prism.(Only for Reference) |
| 激酶实验 | Ub-PLA2 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 fluorescence plate reader. Vehicle (2%(v/v) DMSO) and 10 mM N-ethylmaleimide are included as controls. Where ≥60% inhibition is observed, EC50 values are determined using a sigmoidal dose response equation. |
| 体外活性 | METHODS: HEK293T cells were treated with PR-619 (5-50 µM) for 6 h. Target protein expression levels were measured by Western Blot.
RESULTS: PR-619 interfered with probe labeling at concentrations of 5 µM and above. PR-619 inhibited probe labeling of USP7, but also targeted many other DUBs in the same concentration range, consistent with its broader inhibitory profile. [1]
METHODS: The leukemia cell line K562 was treated with PR-619 (40 µM) for 2 h. Targeting was detected by Immunofluorescence.
RESULTS: PR-619 induced a different distribution of TOP2A and TOP2B fluorescence signals, consisting of large signal foci. FK2 ubiquitin fluorescence signals partially overlapped with those of TOP2A and TOP2B, as well as SUMO2/3. [2] |
| 体内活性 | METHODS: To detect anti-tumor activity in vivo, PR-619 (10 mg/kg once daily) and cisplatin (10 mg/kg three times weekly) were intraperitoneally injected into Nude mice bearing T24 or BFTC-905 xenografts for three weeks.
RESULTS: The combination of cisplatin and PR-619 showed the most significant antitumor effects on T24 and BFTC-905 xenograft tumors compared to monotherapy. [3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : < 1 mg/mL (insoluble）
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| 关键字 | DUBs | PR619 | PR-619 | tau | G0/G1 | Autophagy | Deubiquitinase | ER-stress | ubiquitination | inhibit | Inhibitor | Apoptosis | arrest |
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| 相关库 | DNA 损伤和修复分子库 | 经典已知活性库 | 内质网应激化合物库 | 泛素化化合物库 | HIF-1化合物库 | 自噬库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 细胞周期化合物库 |
United States
