GNE-502

• CAT Number: I045389
• CAS Number: 1953134-16-1
• Molecular Formula: C25H30FN3O3S
• Molecular Weight: 471.59
• Purity: ≥95%
• Synonyms: (1R,3R)-1-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-3-methyl-2-methylsulfonyl-1,3,4,9-tetrahydropyrido[3,4-b]indole
• InChI: InChI=1S/C25H30FN3O3S/c1-17-13-22-21-5-3-4-6-23(21)27-24(22)25(29(17)33(2,30)31)19-7-9-20(10-8-19)32-12-11-28-15-18(14-26)16-28/h3-10,17-18,25,27H,11-16H2,1-2H3/t17-,25-/m1/s1
• InChIKey: ALLRPIPLWLLBGX-CRICUBBOSA-N
• SMILES: CC1CC2=C(C(N1S(=O)(=O)C)C3=CC=C(C=C3)OCCN4CC(C4)CF)NC5=CC=CC=C25

GNE-502 (Cat No.: I045389) is a selective small-molecule inhibitor of the histone methyltransferase PRMT5 (protein arginine methyltransferase 5), an enzyme involved in symmetric dimethylation of arginine residues on histones and other proteins. PRMT5 activity is linked to transcriptional repression, cell proliferation, and oncogenesis, particularly in cancers with MTAP deletions. By inhibiting PRMT5, GNE-502 disrupts aberrant epigenetic regulation, leading to reduced tumor growth. It is primarily used in preclinical research to explore PRMT5’s role in cancer and to evaluate targeted epigenetic therapy strategies.

Reference

[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.
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