PR-619
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.26%
- No. CAS: 2645-32-1
- Fòrmula: C7H5N5S2
- Peso molecular:223.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) PR-619
More- Nat Commun. 2025 May 16;16(1):4564. [Abstract]
- Nat Commun. 2024 Dec 5;15(1):10594. [Abstract]
- Nat Commun. 2024 Jan 2;15(1):9. [Abstract]
- Nat Commun. 2022 Mar 31;13(1):1700. [Abstract]
- Redox Biol. 2026 May:92:104086. [Abstract]
- Mol Cell. 2025 Apr 3:S1097-2765(25)00259-X. [Abstract]
- J Clin Invest. 2022 Sep 1;132(17):e156501. [Abstract]
- Adv Sci (Weinh). 2025 Nov 30:e14349. [Abstract]
- Adv Sci (Weinh). 2025 Aug 30:e09817. [Abstract]
- Sci Adv. 2025 Apr 11;11(15):eadt6159. [Abstract]
- Cell Death Differ. 2023 Jan;30(1):168-183. [Abstract]
- Cell Death Dis. 2023 Dec 7;14(12):802. [Abstract]
- J Immunother Cancer. 2026 Jan 14;14(1):e013498. [Abstract]
- Int J Biol Sci. 2024 Sep 30;20(13):5254-5271. [Abstract]
- Cell Death Discov. 2025 Jul 24;11(1):339. [Abstract]
- Oncogene. 2024 Jun;43(25):1900-1916. [Abstract]
- Int J Biol Macromol. 2025 Oct 13;330(Pt 4):148292. [Abstract]
- EMBO J. 2025 Nov;44(21):5993-6018. [Abstract]
- EMBO J. 2025 Apr;44(8):2211-2231. [Abstract]
- Cell Prolif. 2021 Jan;54(1):e12919. [Abstract]
- J Med Chem. 2022 Oct 27;65(20):13645-13659. [Abstract]
- Cell Mol Life Sci. 2024 May 20;81(1):221. [Abstract]
- Cancer Biol Ther. 2025 Dec;26(1):2459426. [Abstract]
- Virol Sin. 2025 Dec;40(6):910-920. [Abstract]
- FASEB J. 2021 Aug;35(8):e21800. [Abstract]
- Front Biosci (Landmark Ed). 2022 Oct 19;27(10):286. [Abstract]
- PLoS Genet. 2025 Jul 10;21(7):e1011794. [Abstract]
- J Proteome Res. 2025 Dec 5;24(12):6272-6284. [Abstract]
- Anim Cells Syst. 2024 May 11;28(1):237-250. [Abstract]
- Appl Biochem Biotechnol. 2025 Jul 18. [Abstract]
- Cell Biochem Biophys. 2025 Mar;83(1):929-939. [Abstract]
- Cell J. 2023 Feb 1;25(2):118-125. [Abstract]
- bioRxiv. 2026 Jan 20.
- bioRxiv. 2025 May 15:2025.05.11.653360. [Abstract]
- bioRxiv. 2025 March 24.
- bioRxiv. 2025 January 22.
- Research Square Preprint. 2023 Sep 11.
- Ann Transl Med. 2023 Jan 31;11(2):73. [Abstract]
- Patent. US20180263995A1.
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Histological Imaging/Staining
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Actividad biológica
EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1]
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.
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Cell Line:OLN-t40 cells.
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Concentration:0-10 μM.
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Incubation Time:24 hours.
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Result:Exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice[4].
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Dosage:10 mg/kg/day (Cisplatin combined).
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Administration:Intraperitoneally.
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Result:Enhanced the antitumor effect of Cisplatin.
Chemical Information
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No. CAS 2645-32-1
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Appearance Solid
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Peso molecular 223.28
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Fòrmula C7H5N5S2
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Color Light yellow to yellow
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SMILES
NC1=C(SC#N)C=C(SC#N)C(N)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (39)
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Journal Impact Factor
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Most Recent
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Nat Commun
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
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.
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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.
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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
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.
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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
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
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
2025 Mar;83(1):929-939. PMID: 39405024 -
Cell J
2023 Feb 1;25(2):118-125. PMID: 36840458 -
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bioRxiv
2025 May 15:2025.05.11.653360. PMID: 40463042 -
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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 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |