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

PR-619 

Cat. No.: HY-13814 Purity: 98.47%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

PR-619 Chemical Structure

PR-619 Chemical Structure

CAS No. : 2645-32-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 99 In-stock
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10 mg USD 90 In-stock
50 mg USD 245 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

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]

In Vitro

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].

MedChemExpress (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.
In Vivo

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

MedChemExpress (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.
Molecular Weight

223.28

Appearance

Solid

Formula

C7H5N5S2

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.
In Vivo:
  • 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 available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.38%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PR-619
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HY-13814
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