| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GSK503 (GSK-503) is a novel, potent and specific inhibitor of Enhancer of zeste homolog 2 (EZH2) methyltransferase inhibitor with potential antitumor activity. It inhibits EZH2 with Kiapp of 3 to 27 nM. GSK503 demostrates excellent antiproliferative activity and high in vivo antitumor efficacy in a melanoma mouse model.
| ln Vitro |
GSK503, which shares structural similarities with GSK126 and GSK343, inhibits the methyltransferase activity of both wild type and mutant EZH2 with a similar potency (Kiapp=3-27 nM). GSK503 exhibits a selectivity of over 2000 fold over other histone methyltransferases and over 200 fold over EZH1 (Kiapp=636 nM)[1].
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| ln Vivo |
Conditional EZH2 ablation and GSK503 therapy nearly eliminate the production of metastases in a melanoma mouse model while stabilizing the illness through growth inhibition[2]. Normal melanocyte biology is not affected. In mice, GSK503 has good pharmacokinetics. After SRBC or NP-KLH immunization, GSK503 but not the vehicle suppresses the development of the germinal center, phenotyping the Ezh2 null phenotype. GC B-cell counts are decreased by flow cytometry, GC volume and quantity are decreased by immunohistochemistry, and the production of high affinity antibodies is hindered by GSK503 therapy [1].
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| Animal Protocol |
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| References |
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| Additional Infomation |
GSK503 is a potent and specific inhibitor of EZH2 methyltransferase.
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| Molecular Formula |
C31H38N6O2
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| Molecular Weight |
526.67
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| Exact Mass |
526.305
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| CAS # |
1346572-63-1
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| Related CAS # |
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| PubChem CID |
67469117
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| Appearance |
White to gray solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
798.6±60.0 °C at 760 mmHg
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| Flash Point |
436.8±32.9 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
39
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| Complexity |
984
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HRDQQHUKUIKFHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)
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| Chemical Name |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
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| Synonyms |
GSK 503; GSK503; GSK-503
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | |
| 5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8987 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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