BIX 01294

• CAT Number: I005558
• CAS Number: 935693-62-2
• Molecular Formula: C₂₈H₃₈N₆O₂
• Molecular Weight: 490.65
• Purity: ≥95%
• Target: Histone Methyltransferase
• Solubility: DMSO 98 mg/mL; Water 98 mg/mL
• Storage: Store at -20°C
• IC50: 2.7 μM
• IUPAC Name: N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
• InChI: InChI=1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)
• InChIKey: OSXFATOLZGZLSK-UHFFFAOYSA-N
• SMILES: CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC

BIX-01294（Cat No.:I005558） is an inhibitor of G9a Histone Methyltransferase, an enzyme involved in histone methylation and gene regulation. It exhibits an inhibitory concentration (IC50) of 1.9 μM, indicating its potency in suppressing the activity of G9a. By inhibiting G9a, BIX-01294 interferes with the methylation of histones, which can impact gene expression patterns and cellular processes.

Reference

[1]. Kubicek S, O/’Sullivan RJ, August EM et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.


[2]. Chang Y, Zhang X, Horton JR et al. Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16(3):312-7.


[3]. Chang Y, Ganesh T, Horton JR et al.Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases. J Mol Biol. 2010 Jul 2;400(1):1-7.


[4]. Park KE, Johnson CM, Cabot RA. IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo. Reprod Fertil Dev. 2012;24(6):813-21.


[5]. Yang Q, Lu Z, Singh D, Raj JU. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45(4):335-44.