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GSK3368715

Cat. No. M28726

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GSK3368715 Structure
Synonym:

EPZ019997

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Quality Control & Documentation
Biological Activity

GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

Chemical Information
Molecular Weight 366.54
Formula C20H38N4O2
CAS Number 1629013-22-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
References

[1] Anthony B El-Khoueiry, et al. Br J Cancer. Phase 1 study of GSK3368715, a type I PRMT inhibitor, in patients with advanced solid tumors

[2] Andrew Fedoriw, et al. Cancer Immunol Res. Inhibiting Type I Arginine Methyltransferase Activity Promotes T Cell-Mediated Antitumor Immune Responses

[3] Nivine Srour, et al. Cancer Cell. M-TAP Dance: Targeting PRMT1 and PRMT5 Family Members to Push Cancer Cells Over the Edge

[4] Andrew Fedoriw, et al. Cancer Cell. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

[5] Xiao Li, et al. Expert Opin Ther Pat. A patent review of arginine methyltransferase inhibitors (2010-2018)

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Keywords: GSK3368715, EPZ019997 supplier, Histone Methyltransferase, inhibitors, activators

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