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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C7H5N5S2 |
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分子量 | 223.28 | CAS No. | 2645-32-1 | |
Solubility (25°C)* | 体外 | DMSO | 45 mg/mL (201.54 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy. |
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in vitro | PR-619 is a cell-permeable pyridinamine class broad-spectrum DUB inhibitor whose known targets include ATXN3, BAP1, JOSD2, OTUD5, UCH-L1, UCH-L3, UCH-L5/UCH37, USP1, 2, 4, 5, 7, 8, 9X, 10, 14, 15, 16, 19, 20, 22, 24, 28, 47, 48, VCIP135, YOD1, as well as deISGylase PLpro, deNEDDylase DEN1, and deSUMOlyase SENP6. PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 μM, 0.5 to 20 h). PR619 treatment results in upregulation of both K 48 - and K63-linked polyUb chains. PR-619 induces HCT116 cell death with EC50 values of 6.3 μM.[1] |
in vivo | PR-619 enhances the antitumor effect of cisplatin on a cisplatin-naive and cisplatin-resistant UC xenograft of nude mice. |
キナーゼアッセイ | Ub-PLA2 assay | |
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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. | ||
細胞アッセイ | 細胞株 | HCT116, HEK293T |
濃度 | 0.5-50 μM | |
反応時間 | 72 h | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Nude mice |
投薬量 | 10 mg/kg | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Front Pharmacol, 2017, https://doi.org/10.3389/fphar.2017.00565]
Data from [Data independently produced by , , Front Pharmacol, 2018, 8:565]
Data from [Data independently produced by , , Anim Reprod Sci, 2017, 187:64-73]
Noncanonical function of folate through folate receptor 1 during neural tube formation [ Nat Commun, 2024, 15(1):1642] | PubMed: 38388461 |
Precise pancreatic cancer therapy through targeted degradation of mutant p53 protein by cerium oxide nanoparticles [ J Nanobiotechnology, 2023, 21(1):117] | PubMed: 37005668 |
Comparative proteomic and phosphoproteomic analysis reveals differential heat response mechanism in two congeneric oyster species [ Ecotoxicol Environ Saf, 2023, 263:115197] | PubMed: 37451098 |
Ubiquitin-Specific Proteases as Potential Therapeutic Targets in Bladder Cancer-In Vitro Evaluation of Degrasyn and PR-619 Activity Using Human and Canine Models [ Biomedicines, 2023, 10.3390/biomedicines11030759] | PubMed: 36979739 |
A Novel Recognition by the E3 Ubiquitin Ligase of HSV-1 ICP0 Enhances the Degradation of PML Isoform I to Prevent ND10 Reformation in Late Infection [ Viruses, 2023, 15(5)1070] | PubMed: 37243155 |
Ubiquitin-Specific Proteases as Potential Therapeutic Targets in Bladder Cancer-In Vitro Evaluation of Degrasyn and PR-619 Activity Using Human and Canine Models [ Biomedicines, 2023, 11(3)759] | PubMed: 36979739 |
An indispensable role of TAZ in anoikis resistance promoted by OTUB1 deubiquitinating enzyme in basal-like triple-negative breast cancer cells [ Biochem Biophys Res Commun, 2023, 649:1-9] | PubMed: 36738577 |
Depression compromises antiviral innate immunity via the AVP-AHI1-Tyk2 axis [ Cell Res, 2022, 1-17] | PubMed: 35821088 |
Substitution of PINK1 Gly411 modulates substrate receptivity and turnover [ Autophagy, 2022, 1-22.] | PubMed: 36469690 |
Disease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation [ Cell Death Differ, 2022, 10.1038/s41418-022-00983-4] | PubMed: 35379950 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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