1. Cell Cycle/DNA Damage
    Autophagy
  2. Deubiquitinase
    Autophagy
  3. PR-619

PR-619 

製品番号: HY-13814 純度: 98.89%
取扱説明書

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.

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PR-619 構造式

PR-619 構造式

CAS 番号 : 2645-32-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 106 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 96 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 276 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

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.

IC50 & Target

EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1]

体外実験

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].

分子量

223.28

分子式

C₇H₅N₅S₂

CAS 番号

2645-32-1

SMILES

NC1=C(SC#N)C=C(SC#N)C(N)=N1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 21 mg/mL (94.05 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4787 mL 22.3934 mL 44.7868 mL
5 mM 0.8957 mL 4.4787 mL 8.9574 mL
10 mM 0.4479 mL 2.2393 mL 4.4787 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (11.20 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
参考文献
キナーゼ実験
[1]

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].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

細胞実験
[1]

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].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 98.89%

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Keywords:

PR-619PR619PR 619DeubiquitinaseAutophagyDUBsInhibitorinhibitorinhibit

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製品名:
PR-619
製品番号:
HY-13814
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