BIX 01294

• CAT Number: I004323
• CAS Number: 1392399-03-9
• Molecular Formula: C28H38N6O2.3HCl
• Molecular Weight: 600.02
• Purity: ≥95%
• Storage: 3 years-20°Cpowder
• SMILES: CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC.Cl.Cl.Cl

BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.

Reference

[1] Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481.
[2] Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545.
[3] Mabe NW, et al. Cell Rep. 2020 Nov 3;33(5):108341.