DY-46-2

• CAT Number: I042865
• CAS Number: 1105110-83-5
• Molecular Formula: C19H22N6O5S
• Molecular Weight: 446.48
• Purity: ≥95%
• Synonyms: 6-methyl-4-oxo-3-(2-pyrrolidin-1-ylethyl)-N-(6-sulfamoylpyridin-3-yl)furo[2,3-d]pyrimidine-5-carboxamide
• InChI: InChI=1S/C19H22N6O5S/c1-12-15(17(26)23-13-4-5-14(21-10-13)31(20,28)29)16-18(30-12)22-11-25(19(16)27)9-8-24-6-2-3-7-24/h4-5,10-11H,2-3,6-9H2,1H3,(H,23,26)(H2,20,28,29)
• InChIKey: FAZNWIGAOYXZGW-UHFFFAOYSA-N
• SMILES: CC1=C(C2=C(O1)N=CN(C2=O)CCN3CCCC3)C(=O)NC4=CN=C(C=C4)S(=O)(=O)N

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has an inhibitory activity of DNMT3A with an IC50 value of 0.39 μM, which increases linearly with DNA concentration (IDT-01)[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has inhibitory activity against DNMT1, DNMT3B and G9a with IC50 values of 13.0 μM, 105 μM and ＞500 μM, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has cell viability in cancer cells with IC50 values of 0.7 μM, 0.3 μM, 0.7 μM, 0.5 μM, 2.1 μM, 1.7 μM and 91 μM for THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) markedly inhibits the proliferation of cancer cells and shows low cytotoxicity in peripheral blood mononuclear cells (PBMCs)[1].
DY-46-2 (1 μM, 72 h) obviously decreases DNMT3A protein levels, as well as reactive expression of a silenced TSG (p53) in HCT116 cells[1].

Reference

[1]. J. Yu, et al. Discovery of novel non-nucleoside inhibitors with high potency andselectivity for DNA methyltransferase 3A. European Journal of Medicinal Chemistry (2022).