PR-619

製品コードS7130 バッチS713004

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₇H₅N₅S₂

分子量

223.28

CAS No.

2645-32-1

Solubility (25°C)*

体外

DMSO

4 mg/mL (17.91 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PR-619は、deubiquitinylating enzymes (DUBs)の非選択的かつ可逆的阻害剤であり、in vitroアッセイにおけるEC50値は1～20 µMです。PR-619はautophagyを活性化します。
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. This compound is 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). Treatment with this chemical results in upregulation of both K ⁴⁸ - and K⁶³-linked polyUb chains. It induces HCT116 cell death with EC50 values of 6.3 μM.
in vivo	PR-619 enhances the antitumor effect on UC xenograft of nude mice.

プロトコル(参考用のみ)

キナーゼアッセイ	Ub-PLA₂ assay
キナーゼアッセイ	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.
動物実験	動物モデル	Nude mice
	投薬量	10 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/22118674/
https://pubmed.ncbi.nlm.nih.gov/31627336/

カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

USP15 Facilitates Colorectal Cancer Immune Evasion through SMYD3/CCL2-Dependent Myeloid-Derived Suppressor Cell Recruitment [ Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194]	PubMed: 40323348
A novel mechanism in regulating drug sensitivity, growth, and apoptosis of bortezomib-resistant multiple myeloma cells: the USP4/KLF2/HMGA2 cascade [ J Orthop Surg Res, 2025, 20(1):220]	PubMed: 40022160
Linear ubiquitination prevents lipodystrophy and obesity-associated metabolic syndrome [ Sci Adv, 2025, 11(38):eadw2539]	PubMed: 40961178
Noncanonical function of folate through folate receptor 1 during neural tube formation [ Nat Commun, 2024, 15(1):1642]	PubMed: 38388461
Sugar-mediated non-canonical ubiquitination impairs Nrf1/NFE2L1 activation [ Mol Cell, 2024, 84(16):3115-3127.e11]	PubMed: 39116872
Increased CSN5 expression enhances the sensitivity to lenalidomide in multiple myeloma cells [ iScience, 2024, 27(12):111399]	PubMed: 39687025
MAPK-dependent control of mitotic progression in S. pombe [ BMC Biol, 2024, 22(1):71]	PubMed: 38523261
DNA polymerase η is regulated by mutually exclusive mono-ubiquitination and mono-NEDDylation [ bioRxiv, 2024, 2024.10.12.618026]	PubMed: 39416117
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

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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