Free shipping on all orders over $ 500

GSK3368715

Cat. No. M28726

All AbMole products are for research use only, cannot be used for human consumption.

GSK3368715 Structure
Synonym:

EPZ019997

Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?
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)

Related Histone Methyltransferase Products
MS67 

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM.
MS8511 

MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP).
TM2-115 

TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.
(R)-HH2853 

(R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F.
G9a-IN-1 

G9a-IN-1 is a G9a protein inhibitor.
  Catalog
Abmole Inhibitor Catalog




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

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.


 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.