UNC0379

• CAT Number: I002080
• CAS Number: 1620401-82-2
• Molecular Formula: C₂₃H₃₅N₅O₂
• Molecular Weight: 413.56
• Purity: ≥95%
• Target: HMTase
• Solubility: 10 mM in DMSO
• Storage: Desiccate at -20C
• IC50: 7.3±1.0 uM
• InChI: InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)
• InChIKey: WEXCGGWTIDNVNT-UHFFFAOYSA-N
• SMILES: COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCCC3)NCCCCCN4CCCC4)OC

UNC0379 (CAT: I002080) is a selective inhibitor of the lysine methyltransferase SETD8. It acts as a substrate-competitive inhibitor, specifically targeting the catalytic activity of SETD8. By inhibiting SETD8, UNC0379 can modulate the methylation of histone H4 at lysine 20 (H4K20), which is a critical epigenetic modification involved in gene expression regulation. The selective inhibition of SETD8 by UNC0379 offers potential for studying the role of SETD8-mediated methylation in cellular processes and for developing therapeutic strategies targeting SETD8 in diseases where dysregulation of H4K20 methylation is implicated.

Reference

[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.