| Name | GSK503 |
| Description | GSK-503, a potent EZH2 inhibitor, has potential antitumor activity. |
| 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. |
| 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] |
| 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)
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| Keywords | GSK503 | Inhibitor | inhibit | GSK-503 | GSK 503 | Histone Methyltransferase |
| Inhibitors Related | BIX-01294 trihydrochloride | Tazemetostat | Piribedil | XY1 | UNC 0631 | GSK126 | MAK683 | EZM 2302 | EPZ015666 | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Chromatin Modification Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
