GSK503

Catalog No.S7804 Batch:S780402

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Technical Data

Formula

C31H38N6O2
Molecular Weight 526.67 CAS No. 1346572-63-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (189.87 mM)
Ethanol 4 mg/mL (7.59 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
Targets
EZH2 [1]
8 nM
In vitro GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition and the effects are enhanced by 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]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Animal Study:[1]
  • Animal Models

    Male SCID mice bearing SUDHL4 and SUDHL6 tumors

  • Dosages

    150 mg/kg daily

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , J Pathol, 2018, 245(4):433-444]

Selleck's GSK503 has been cited by 7 publications

Study on the Effect of EZH2 Inhibitor Combined with TIGIT Monoclonal Antibody against Multiple Myeloma Cells [ Int J Mol Sci, 2023, 24(10)8603] PubMed: 37239949
PRC2-mediated epigenetic suppression of type I IFN-STAT2 signaling impairs antitumor immunity in luminal breast cancer [ Cancer Res, 2022, CAN-22-0736] PubMed: 36222718
EZH2-mediated H3K27me3 is a predictive biomarker and therapeutic target in uveal melanoma [ Front Genet, 2022, 13:1013475] PubMed: 36276954
An Evolutionarily Conserved Function of Polycomb Silences the MHC Class I Antigen Presentation Pathway and Enables Immune Evasion in Cancer. [ Cancer Cell, 2019, 36(4):385-401] PubMed: 31564637
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
Overexpression of EZH2 in conjunctival melanoma offers a new therapeutic target [Cao J, et al. J Pathol, 2018, 245(4):433-444] PubMed: 29732557
Human Papillomavirus Downregulates the Expression of IFITM1 and RIPK3 to Escape from IFNγ- and TNFα-Mediated Antiproliferative Effects and Necroptosis. [Ma W, et al. Front Immunol, 2016, 7:496] PubMed: 27920775

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.