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GSK503

Catalog No. T1775   CAS 1346572-63-1

GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.

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GSK503 Chemical Structure
GSK503, CAS 1346572-63-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 113.00
25 mg In stock $ 219.00
50 mg In stock $ 396.00
100 mg In stock $ 589.00
500 mg In stock $ 1,280.00
1 mL * 10 mM (in DMSO) In stock $ 84.00
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Purity: 99.74%
Purity: 99.54%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
Targets&IC50 EZH2:8 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]
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

Solubility Information

DMSO: 93 mg/mL (176.6 mM)

Ethanol: 25 mg/mL (47.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Béguelin W, et al. Cancer Cell. 2013, 23(5), 677-692 2. Zingg D, et al. Nat Commun. 2015, 6, 6051.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Compound Library Reprogramming Compound Library Bioactive Compounds Library Max Methylation Compound Library Histone Modification Compound Library Anti-Aging Compound Library Inhibitor Library Bioactive Compound Library Epigenetics Compound Library

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Keywords

GSK503 1346572-63-1 Chromatin/Epigenetic Histone Methyltransferase Inhibitor inhibit GSK-503 GSK 503 inhibitor

 

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