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GSK503
🥰Excellent
Catalog No. T1775Cas No. 1346572-63-1
GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
GSK503
🥰Excellent
Purity: 99.74%
Catalog No. T1775Cas No. 1346572-63-1
GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $31 | In Stock | |
| 2 mg | $44 | In Stock | |
| 5 mg | $72 | In Stock | |
| 10 mg | $113 | In Stock | |
| 25 mg | $219 | In Stock | |
| 50 mg | $396 | In Stock | |
| 100 mg | $589 | In Stock | |
| 500 mg | $1,280 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $84 | In Stock |
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Purity:99.74%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK-503, a potent EZH2 inhibitor, has potential antitumor activity. |
| Targets&IC50 | EZH2:8 nM |
| In vitro | GSK503 inhibits the methyltransferase activity of both WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition, with enhanced effects when combined with ABT737 or Obatoclax. [1] |
| In vivo | In C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. [1] In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation. [2] |
| Kinase Assay | In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively. |
| Molecular Weight | 526.67 |
| Formula | C31H38N6O2 |
| Cas No. | 1346572-63-1 |
| Smiles | CC(C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCN(C)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O |
| Relative Density. | 1.24 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 93 mg/mL (176.6 mM) Ethanol: 25 mg/mL (47.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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