PRT4165
Based on 10 publication(s) in Google Scholar
PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 31083-55-3
- Formel: C15H9NO2
- Molecular Weight:235.24
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) PRT4165
More- Cancer Res. 2018 Jan 1;78(1):51-63. [Abstract]
- Clin Cancer Res. 2024 Nov 15;30(22):5166-5179. [Abstract]
- Cell Death Dis. 2021 Jun 12;12(6):610. [Abstract]
- Stem Cell Reports. 2025 Dec 26:102756. [Abstract]
- Clin Epigenetics. 2022 Dec 24;14(1):184. [Abstract]
- FEBS J. 2023 Jul;290(14):3629-3645. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Res Sq. 2025 Dec 17.
- University of Washington. 2025.
- Research Square Print. 2022 May.
Customer Validation & Images
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IF
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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RT-PCR
Biologische Aktivität
PRC1[1]
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Cell Line
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Type | Value | Description | References |
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| U2OS | IC50 |
45.2 μM
Compound: 1; PRT4165
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Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs
Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs
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[PMID: 38636717] |
PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation. In vitro E3 ubiquitin ligase activity assays reveal that PRT4165 inhibits both RNF2 and RING 1A, but not RNF8 nor RNF168. In the presence of PRT4165, H2A ubiquitylation can be completely inhibited regardless of whether RING1 or RNF2 contributes the E3 ubiquitin ligase activity. Treatment of cells for 60 min with 50 μM PRT4165 results in a dramatic reduction in total ubiquitylated histone H2A. It is also found that longer exposure of the cells with the PRT4165 (30 and 60 min) leads to increased levels of γ-H2AX in unirradiated cells. PRT4165 inhibits double-strand break (DSB) repair at the 8-h time point compare with mock treated cells. Cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 31083-55-3
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Appearance Solid
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Molecular Weight 235.24
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Formel C15H9NO2
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Color Light green to green
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SMILES
O=C1/C(C(C2=C1C=CC=C2)=O)=C/C3=CC=CN=C3
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Synonyms
NSC600157
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Res
CBX8 Exhibits Oncogenic Activity via AKT/β-Catenin Activation in Hepatocellular Carcinoma. [Abstract]2018 Jan 1;78(1):51-63. PMID: 29066512
PRT4165 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2018 Jan 1;78(1):51-63. [Abstract]
Bel-7402 and SMMC-7721 cells with CBX8 overexpression were treated with Ring1b siRNA or RING inhibitor PRT4165 for 24 hours. The mRNA expression of EGR1 was determined by qRT-PCR.
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Clin Cancer Res
Epigenome Reprogramming Through H3K27 and H3K4 Trimethylation as a Resistance Mechanism to DNA Methylation Inhibition in BRAFV600E-Mutated Colorectal Cancer. [Abstract]2024 Nov 15;30(22):5166-5179. PMID: 39269307
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Nov 15;30(22):5166-5179. [Abstract]
Cell viability (relative to DMSO control) 72 hours after treatment by either DNMSO, 5-azacitidine (AZA; 1μM), EPZ-6438 (EPZ; 60μM), GSK126 (GSK; 25μM), PRT4165 (PRT; 20μM), or combinations of inhibitors with 5-azacitidine in RKO cell line.
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Nov 15;30(22):5166-5179. [Abstract]
B1003 cell lines for 10 days (5-azacitidine (0.1μM); EPZ-6438 (30μM), GSK126 (3μM), PRT4165 (10μM)).
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Cell Death Dis
G-protein-coupled receptor GPR17 inhibits glioma development by increasing polycomb repressive complex 1-mediated ROS production. [Abstract]2021 Jun 12;12(6):610. PMID: 34120140 -
Stem Cell Reports
2025 Dec 26:102756. PMID: 41455470
PRT4165 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2025 Dec 26:102756. [Abstract]
Whole-mount IF analysis demonstrated that treatment with a combination of PRC1/2 inhibitors ([PRCis] EED226 + PRT4165 + GSK126) significantly increased SOX2+ /K8+ MCs approximately 2-fold compared to the vehicle group treated with an equal volume of DMSO. Following 6 days treatment with vehicle (DMSO) or PRCi (10 μM EED +10 μM PRT4165 + 5 μM GSK126) on vibrissae of mice at E14.5, whole-mount IF staining for SOX2 (magenta) and K8 (yellow) was performed.
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Clin Epigenetics
Identification of hepatocellular carcinoma subtypes based on PcG-related genes and biological relevance with cancer cells. [Abstract]2022 Dec 24;14(1):184. PMID: 36566204
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2022 Dec 24;14(1):184. [Abstract]
The downregulation of H3K27me3 and H2AK119ub protein level in HCC cells after GSK126 or PRT4165 (10 μM; 24 h) treatment.
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2022 Dec 24;14(1):184. [Abstract]
The downregulation of three fatty acid oxidation-related genes mRNA expression in HCC cells after GSK126 or PRT4165 (10 μM) treatment. β-actin (ACTB) was used as internal control.
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2022 Dec 24;14(1):184. [Abstract]
The lipid fluorescence staining of HCC cells after GSK126 or PRT4165 (10 μM; 24 h) treatment.
PRT4165 purchased from MedChemExpress. Usage Cited in: Clin Epigenetics. 2022 Dec 24;14(1):184. [Abstract]
Cell apoptosis rate of HCC cell after oxaliplatin treatment (5 μg/ml) with GSK126 or PRT4165 (10 μM; 24 h) measured by flow cytometry.
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FEBS J
Radiation resistance of cancer cells caused by mitochondrial dysfunction depends on SIRT3-mediated mitophagy. [Abstract]2023 Jul;290(14):3629-3645. PMID: 36871142 -
Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
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Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (106.27 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (10.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (10.63 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protokoll
Cells are treated with different concentrations of the PRT4165 60 min prior to irradiation (2 Gy). The cells are harvested 2 h after IR. The cells are washed with PBS twice and then fixed with 1% paraformaldehyde at 37°C for 10 min. After cooling on ice for 1 min, the cells are permeabilized with 90% methanol and stored at -20°C overnight. Fixed cells are washed with PBS twice and blocked with FACS incubation buffer (0.5% BSA in PBS) for 10 min. The cells are then stained with anti-phosphohistone H3 (serine 10) antibody at 1:500 dilution in FACS incubation buffer for 1 h at room temperature[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2510 mL | 21.2549 mL | 42.5098 mL | 106.2744 mL |
| 5 mM | 0.8502 mL | 4.2510 mL | 8.5020 mL | 21.2549 mL | |
| 10 mM | 0.4251 mL | 2.1255 mL | 4.2510 mL | 10.6274 mL | |
| 15 mM | 0.2834 mL | 1.4170 mL | 2.8340 mL | 7.0850 mL | |
| 20 mM | 0.2125 mL | 1.0627 mL | 2.1255 mL | 5.3137 mL | |
| 25 mM | 0.1700 mL | 0.8502 mL | 1.7004 mL | 4.2510 mL | |
| 30 mM | 0.1417 mL | 0.7085 mL | 1.4170 mL | 3.5425 mL | |
| 40 mM | 0.1063 mL | 0.5314 mL | 1.0627 mL | 2.6569 mL | |
| 50 mM | 0.0850 mL | 0.4251 mL | 0.8502 mL | 2.1255 mL | |
| 60 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7712 mL | |
| 80 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3284 mL | |
| 100 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL | 1.0627 mL |
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