1. Cell Cycle/DNA Damage
    Autophagy
    Apoptosis
  2. Deubiquitinase
    Autophagy
    Apoptosis
  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 and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.

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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  
Solution
10 mM * 1 mL in DMSO USD 106 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 106 在庫あり
Estimated Time of Arrival: December 31
Solid
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 2 publication(s) in Google Scholar

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製品説明

PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis[1][2][3][4].

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[2].
PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau[3].
PR-619 (7-12.5 μM) causes an increase in the abundance of ubiquitinated proteins within 24 h. PR-619 leads to the induction of heat shock proteins and to an increase of ubiquitinated proteins[3].
PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells[3].
PR-619 (5, 7.5, and 10 μM) induces ER Stress and ER-Stress related apoptosis on T24 and BFTC-905 cells. PR-619 induces polyubiquitination, Bcl-2 downregulation, and concurrent PARP cleavage in a dose-dependent manner. PR-619 induces G0/G1 arrest in UC cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: OLN-t40 cells.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM.
体内実験

PR-619 (10 mg/kg/day) enhances the antitumor effect of Cisplatin on a Cisplatin-Naïve and Cisplatin-resistant UC Xenograft of nude mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice[4].
Dosage: 10 mg/kg/day (Cisplatin combined).
Administration: Intraperitoneally.
Result: Enhanced the antitumor effect of Cisplatin.
分子量

223.28

分子式

C₇H₅N₅S₂

CAS 番号
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

純度: 98.89%

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Keywords:

PR-619PR619PR 619DeubiquitinaseAutophagyApoptosisDUBsG0/G1arrestER-stresstauubiquitinationInhibitorinhibitorinhibit

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製品名:
PR-619
製品番号:
HY-13814
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