BI-9321

• CAT Number: I017236
• CAS Number: 2387510-86-1
• Molecular Formula: C₂₂H₂₁FN₄
• Molecular Weight: 360.43
• Purity: ≥95%
• Target: Histone Methyltransferase
• IUPAC Name: [4-[5-(7-fluoroquinolin-4-yl)-1-methylimidazol-4-yl]-3,5-dimethylphenyl]methanamine
• InChI: InChI=1S/C22H21FN4/c1-13-8-15(11-24)9-14(2)20(13)21-22(27(3)12-26-21)18-6-7-25-19-10-16(23)4-5-17(18)19/h4-10,12H,11,24H2,1-3H3
• InChIKey: WOAOENGFAAUUGT-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC(=C1C2=C(N(C=N2)C)C3=C4C=CC(=CC4=NC=C3)F)C)CN

BI-9321(CAT: I017236) is a potent and selective antagonist of the nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain, with a K value of 166 nM. It disrupts histone interactions at the methyl-lysine binding site of the PWWP1 domain, exhibiting sub-micromolar in vitro activity and cellular engagement at 1 μM. In U2OS cells, it achieves an IC50 of 1.2 μM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2, highlighting its specificity. As a single agent, it downregulates Myc mRNA expression and reduces cell proliferation in MOLM-13 leukemia cells. BI-9321 is a valuable tool in epigenetics and oncology research, particularly for exploring NSD3-driven cancer pathways and developing targeted therapies.