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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 |
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 |
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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