Name: PR-619
Brand: Selleck Chemicals
SKU: S7130
Availability: InStock
Rating: 5 (64 reviews)

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Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	Proteasome E1 Activating E3 Ligase p97 SUMO E2 conjugating
Other DUB Inhibitors	P5091 IU1 b-AP15 P22077 ML323 LDN-57444 VLX1570 TCID EOAI3402143 USP25/28 inhibitor AZ1

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (13.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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.
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	223.28	Formula	C₇H₅N₅S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2645-32-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=C(C(=NC(=C1SC#N)N)N)SC#N

Mechanism of Action

Targets/IC₅₀/Ki	JOSD2 (Cell-free assay) 1.17 μM(EC50) SENP6 core (Cell-free assay) 2.37 μM(EC50) UCH-L3 (Cell-free assay) 2.95 μM(EC50) USP4 (Cell-free assay) 3.93 μM(EC50) USP8 (Cell-free assay) 4.90 μM(EC50) DEN1 (Cell-free assay) 4.98 μM(EC50) USP20 (Cell-free assay) 5.10 μM(EC50) USP28 (Cell-free assay) 6.24 μM(EC50) USP7 (Cell-free assay) 6.86 μM(EC50) USP2 core (Cell-free assay) 7.20 μM(EC50) USP15 (Cell-free assay) 8.23 μM(EC50) USP5 (Cell-free assay) 8.61 μM(EC50) USP47 (Cell-free assay) 8.87 μM(EC50) UCH-L5 (Cell-free assay) 9.26 μM(EC50) UCH-L1 (Cell-free assay) 12.8 μM(EC50) Plpro (Cell-free assay) 14.2 μM(EC50) PLA2 (Cell-free assay) >50 μM(EC50) Calpain 1 (Cell-free assay) >50 μM(EC50) CT-L (Cell-free assay) >50 μM(EC50) Cathepsin D (Cell-free assay) >50 μM(EC50) MMP13 (Cell-free assay) >50 μM(EC50) Trypsin (Cell-free assay) >50 μM(EC50)
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.
Kinase Assay	Ub-PLA₂ assay
Kinase Assay	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.
In vivo	PR-619 enhances the antitumor effect on UC xenograft of nude mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22118674/ [2] https://pubmed.ncbi.nlm.nih.gov/31627336/

Applications

Methods	Biomarkers	Images	PMID
Western blot	FOXM1		30865895

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PR-619 DUB inhibitor

Chemical Structure

Molecular Weight: 223.28