GSK503
Based on 8 publication(s) in Google Scholar
GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
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- Pureza: 99.52%
- No. CAS: 1346572-63-1
- Fòrmula: C31H38N6O2
- Peso molecular:526.67
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK503
More- Nat Commun. 2025 Mar 18;16(1):2663. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- PLoS Pathog. 2020 Mar 24;16(3):e1008429. [Abstract]
- Int Immunopharmacol. 2023 Sep 12;124(Pt A):110918. [Abstract]
- Exp Eye Res. 2023 Feb:227:109389. [Abstract]
- bioRxiv. 2025 May 4:2025.04.29.651320. [Abstract]
- Patent. US20180263995A1.
- Oncotarget. 2017 Apr 25;8(35):58654-58667. [Abstract]
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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EZH2 |
GSK503 inhibits the methyltransferase activity of wild type and mutant EZH2 with similar potency (Kiapp=3-27 nM) and is structurally related to GSK126 and GSK343. GSK503 is >200 fold selective over EZH1 (Kiapp=636 nM) and >4000 fold selective over other histone methyltransferases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1346572-63-1
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Appearance Solid
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Peso molecular 526.67
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Fòrmula C31H38N6O2
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Color White to gray
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SMILES
O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O
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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 (8)
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Journal Impact Factor
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Most Recent
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Nat Commun
HSD17B4 deficiency causes dysregulation of primary cilia and is alleviated by acetyl-CoA. [Abstract]2025 Mar 18;16(1):2663. PMID: 40102401 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
PLoS Pathog
BRD4 inhibition exerts anti-viral activity through DNA damage-dependent innate immune responses. [Abstract]2020 Mar 24;16(3):e1008429. PMID: 32208449 -
Int Immunopharmacol
Attenuated Salmonella-delivered PD-1 siRNA enhances the antitumor effects of EZH2 inhibitors in colorectal cancer. [Abstract]2023 Sep 12;124(Pt A):110918. PMID: 37708707 -
Exp Eye Res
2023 Feb:227:109389. PMID: 36669714 -
bioRxiv
2025 May 4:2025.04.29.651320. PMID: 40654780 -
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Oncotarget
The long noncoding RNA HOTAIR activates the Hippo pathway by directly binding to SAV1 in renal cell carcinoma. [Abstract]2017 Apr 25;8(35):58654-58667. PMID: 28938586
GSK503 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Apr 25;8(35):58654-58667. [Abstract]
Treatment of RCC cells with an EZH2 inhibitor (GSK503) upregulates modulators of the Hippo pathway and SAV1 expression at the mRNA and protein levels.
Solvente y solubilidad
DMSO : ≥ 44 mg/mL (83.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (4.75 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 (4.75 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 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.
Protocolo
Mice: To pharmacologically inhibit Ezh2 activity, Tyr::N-RasQ61K Ink4a-/- and C57Bl/6 mice are subjected to treatment with GSK503, which is diluted (15 mg/mL) in 20% Captisol solution. Efficient Ezh2 inhibition is achieved by daily intraperitoneal injections of 150 mg/kg GSK503 over 35 consecutive days. Mice are monitored during and after treatment to measure GSK503-induced reversible weight loss. C57Bl/6 and Foxn1nu/nu mice engrafted with melanoma cells are subjected to TM and GSK503 treatment as described above[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Béguelin W, et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell. 2013 May 13;23(5):677-92. [Content Brief]
[2]. Zingg D, et al. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. Nat Commun. 2015 Jan 22;6:6051. [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 | 1.8987 mL | 9.4936 mL | 18.9872 mL | 47.4681 mL |
| 5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | 9.4936 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8987 mL | 4.7468 mL | |
| 15 mM | 0.1266 mL | 0.6329 mL | 1.2658 mL | 3.1645 mL | |
| 20 mM | 0.0949 mL | 0.4747 mL | 0.9494 mL | 2.3734 mL | |
| 25 mM | 0.0759 mL | 0.3797 mL | 0.7595 mL | 1.8987 mL | |
| 30 mM | 0.0633 mL | 0.3165 mL | 0.6329 mL | 1.5823 mL | |
| 40 mM | 0.0475 mL | 0.2373 mL | 0.4747 mL | 1.1867 mL | |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3797 mL | 0.9494 mL | |
| 60 mM | 0.0316 mL | 0.1582 mL | 0.3165 mL | 0.7911 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2373 mL | 0.5934 mL |
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