Art. -Nr.: HY-13814

PR-619

39 Cited Publications

Kundenbewertung

Based on 39 publication(s) in Google Scholar

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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Reinheit: 99.26%
CAS. Nr.: 2645-32-1
Formel: C₇H₅N₅S₂
Molecular Weight:223.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PR-619 Chemical Structure

CAS. Nr.: 2645-32-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (39)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 2645-32-1
Appearance Solid
Molecular Weight 223.28
Formel C₇H₅N₅S₂
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (39)

All WBHistological Imaging/StainingIP

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Journal Impact Factor

Nat Commun

USP2 inhibition unleashes CD47-restrained phagocytosis and enhances anti-tumor immunity. [Abstract]

2025 May 16;16(1):4564. PMID: 40379682
Nat Commun

CDK9 recruits HUWE1 to degrade RARα and offers therapeutic opportunities for cutaneous T-cell lymphoma. [Abstract]

2024 Dec 5;15(1):10594. PMID: 39632829
Nat Commun

Pharmaceutical targeting of OTUB2 sensitizes tumors to cytotoxic T cells via degradation of PD-L1. [Abstract]

2024 Jan 2;15(1):9. PMID: 38167274
Nat Commun

USP8 inhibition reshapes an inflamed tumor microenvironment that potentiates the immunotherapy. [Abstract]

2022 Mar 31;13(1):1700. PMID: 35361799
Redox Biol

USP20 governs tyrosine kinase inhibitors resistance through ferroptosis evasion by targeting GPX4 in cancers. [Abstract]

2026 May:92:104086. PMID: 41844497
Mol Cell

MLKL activity requires a splicing-regulated, druggable intramolecular interaction. [Abstract]

2025 Apr 3:S1097-2765(25)00259-X. PMID: 40209701
J Clin Invest

Human β-defensin-3 attenuates atopic dermatitis-like inflammation through autophagy activation and the aryl hydrocarbon receptor signaling pathway. [Abstract]

2022 Sep 1;132(17):e156501. PMID: 35834333
Adv Sci (Weinh)

Microcystin-LR Triggers Renal Tubular Ferroptosis Through Epigenetic Repression of GPX4: Implications for Environmental Nephrotoxicity. [Abstract]

2025 Nov 30:e14349. PMID: 41319283
Adv Sci (Weinh)

K29-Linked Ubiquitination of Transcription Regulators Controls Cell Proliferation in the Unfolded Protein Response. [Abstract]

2025 Aug 30:e09817. PMID: 40884253
Sci Adv

The cohesin-associated protein Pds5A governs the meiotic spindle assembly via deubiquitination of Kif5B in oocytes. [Abstract]

2025 Apr 11;11(15):eadt6159. PMID: 40215310
Cell Death Differ

FAAH served a key membrane-anchoring and stabilizing role for NLRP3 protein independently of the endocannabinoid system. [Abstract]

2023 Jan;30(1):168-183. PMID: 36104448

PR-619 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):168-183. [Abstract]

Immunoblot analysis of NLRP3 and GAPDH in LPS-primed (Mock) FAAH-/- BMDMs, with or without co-treatment of PYR41 (5 μM) or PR619 (5 μM).

PR-619 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):168-183. [Abstract]

Immunoblotting analysis showing the protein levels of Kif5B in control, PR-619-treated.PR-619 (10 μM) was used to treat GV oocytes for 22 hours, respectively.
Cell Death Dis

POU5F1 promotes the proliferation, migration, and invasion of gastric cancer cells by reducing the ubiquitination level of TRAF6. [Abstract]

2023 Dec 7;14(12):802. PMID: 38062041
J Immunother Cancer

CD47 destabilization via manipulating the SPOP-USP2 axis augments macrophage phagocytosis and cancer immunotherapy. [Abstract]

2026 Jan 14;14(1):e013498. PMID: 41534899
Int J Biol Sci

Amlexanox Enforces Osteogenic Differentiation and Bone Homeostasis Through Inhibiting Ubiquitin-Dependent Degradation of β-Catenin. [Abstract]

2024 Sep 30;20(13):5254-5271. PMID: 39430247

PR-619 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Sep 30;20(13):5254-5271. [Abstract]

C3H/10T1/2 cells pre-treated with AM were intervened with CHX in the presence of or PR-619 (15 μM, 48 h).

PR-619 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Sep 30;20(13):5254-5271. [Abstract]

C3H/10T1/2 cells were co-incubated with or without AM in the presence of PR-619 for 48 hours, followed by IP with anti-β-catenin and IB with indicated antibodies.
Cell Death Discov

The RNF8/OPTN/KDM6A axis controls macrophage polarization to maintain testicular microenvironment homeostasis. [Abstract]

2025 Jul 24;11(1):339. PMID: 40707433
Oncogene

The DNA damage-independent ATM signalling maintains CBP/DOT1L axis in MLL rearranged acute myeloid leukaemia. [Abstract]

2024 Jun;43(25):1900-1916. PMID: 38671157
Int J Biol Macromol

CLIC1 regulates cellular oxidative stress and gastric cancer progress by enhancing ACOX1 ubiquitination. [Abstract]

2025 Oct 13;330(Pt 4):148292. PMID: 41093222
EMBO J

RNF114 and RNF166 exemplify reader-writer E3 ligases that extend K11 polyubiquitin onto sites of MARUbylation. [Abstract]

2025 Nov;44(21):5993-6018. PMID: 41039157
EMBO J

Ubiquitin is directly linked via an ester to protein-conjugated mono-ADP-ribose. [Abstract]

2025 Apr;44(8):2211-2231. PMID: 40000907
Cell Prolif

Inhibition of deubiquitination by PR-619 induces apoptosis and autophagy via ubi-protein aggregation-activated ER stress in oesophageal squamous cell carcinoma. [Abstract]

2021 Jan;54(1):e12919. PMID: 33129231
J Med Chem

Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]

2022 Oct 27;65(20):13645-13659. PMID: 36221183
Cell Mol Life Sci

P62 promotes FSH-induced antral follicle formation by directing degradation of ubiquitinated WT1. [Abstract]

2024 May 20;81(1):221. PMID: 38763964

PR-619 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 May 20;81(1):221. [Abstract]

The hematoxylin-stained ovary sections of control and PR-619 (75 µM, 48 h) mice. The boxed region of each figure was magnified accordingly. Scale bar: 100 μm.
Cancer Biol Ther

Caspase 3-specific cleavage of ubiquitin-specific peptidase 48 enhances drug-induced apoptosis in AML. [Abstract]

2025 Dec;26(1):2459426. PMID: 39878157
Virol Sin

Ubiquitin-specific protease 5 promotes EV-A71 replication by de-ubiquitinating MAVS and IRF3. [Abstract]

2025 Dec;40(6):910-920. PMID: 41352537
FASEB J

Cullin 2-RBX1 E3 ligase and USP2 regulate antithrombin ubiquitination and stability. [Abstract]

2021 Aug;35(8):e21800. PMID: 34324733
Front Biosci (Landmark Ed)

The Deubiquitinating Enzyme USP4 Functions as an Oncoprotein in Gastric Cancer and Mediates NF-κB Signaling by Regulating PRL-3 Expression. [Abstract]

2022 Oct 19;27(10):286. PMID: 36336860
PLoS Genet

Nuclear p62/SQSTM1 facilitates ubiquitin-independent proteasomal degradation of BMAL1. [Abstract]

2025 Jul 10;21(7):e1011794. PMID: 40638681
J Proteome Res

Proteomics Combined with N-Glycoproteomics to Explore the Pathogenesis of Nasopharyngeal Carcinoma. [Abstract]

2025 Dec 5;24(12):6272-6284. PMID: 41269767
Anim Cells Syst

Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]

2024 May 11;28(1):237-250. PMID: 38741950
Appl Biochem Biotechnol

USP7 Stabilizes USF1 to Aggravate ox-LDL-Induced Endothelial Injury Through the MYD88/NF-κB Pathway in Atherosclerosis. [Abstract]

2025 Jul 18. PMID: 40679551
Cell Biochem Biophys

The Deubiquitinating Enzyme USP4 Promotes Trophoblast Dysfunction by Stabilizing RYBP. [Abstract]

2025 Mar;83(1):929-939. PMID: 39405024
Cell J

High Expression of G9a Induces Cisplatin Resistance in Hepatocellular Carcinoma. [Abstract]

2023 Feb 1;25(2):118-125. PMID: 36840458
bioRxiv

2026 Jan 20.
bioRxiv

A family of E3 ligases extend K11 polyubiquitin on sites of MARUbylation. [Abstract]

2025 May 15:2025.05.11.653360. PMID: 40463042
bioRxiv

2025 March 24.
bioRxiv

2025 January 22.
Research Square Preprint

2023 Sep 11.
Ann Transl Med

Hydrogen sulfide alleviates ischemia induced liver injury by repressing the SPHK1/S1P pathway. [Abstract]

2023 Jan 31;11(2):73. PMID: 36819566
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (89.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12. [Content Brief]

[2]. Bertuccio CA, et al. Anterograde trafficking of KCa3.1 in polarized epithelia is Rab1- and Rab8-dependent and recycling endosome-independent. PLoS One. 2014 Mar 14;9(3):e92013. [Content Brief]

[3]. Seiberlich V, et al. The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases. Biochim Biophys Acta. 2012 Nov;1823(1 [Content Brief]

[4]. Kuan-Lin Kuo, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: In Vitro and In Vivo Study. Cells. 2019 Oct 17;8(10):1268. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.4787 mL	22.3934 mL	44.7868 mL	111.9670 mL
	5 mM	0.8957 mL	4.4787 mL	8.9574 mL	22.3934 mL
	10 mM	0.4479 mL	2.2393 mL	4.4787 mL	11.1967 mL
	15 mM	0.2986 mL	1.4929 mL	2.9858 mL	7.4645 mL
	20 mM	0.2239 mL	1.1197 mL	2.2393 mL	5.5984 mL
	25 mM	0.1791 mL	0.8957 mL	1.7915 mL	4.4787 mL
	30 mM	0.1493 mL	0.7464 mL	1.4929 mL	3.7322 mL
	40 mM	0.1120 mL	0.5598 mL	1.1197 mL	2.7992 mL
	50 mM	0.0896 mL	0.4479 mL	0.8957 mL	2.2393 mL
	60 mM	0.0746 mL	0.3732 mL	0.7464 mL	1.8661 mL
	80 mM	0.0560 mL	0.2799 mL	0.5598 mL	1.3996 mL

Keywords

PR-619

39 Cited Publications

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PR-619

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Aging Compound Library Mini

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) PR-619

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (39)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PR-619

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Aging Compound Library Mini

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) PR-619

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (39)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PR-619 Related Classifications

HY-13814 Related Classifications