PBRM1-BD2-IN-8

• CAT Number: I042609
• CAS Number: 2819989-75-6
• Molecular Formula: C15H13BrN2O
• Molecular Weight: 317.18
• Purity: ≥95%
• Synonyms: 5-bromo-2-(3-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one
• InChI: InChI=1S/C15H13BrN2O/c1-9-4-2-5-10(8-9)14-17-12-7-3-6-11(16)13(12)15(19)18-14/h2-8,14,17H,1H3,(H,18,19)
• InChIKey: PXWIXTCIXZCREB-UHFFFAOYSA-N
• SMILES: CC1=CC(=CC=C1)C2NC3=C(C(=CC=C3)Br)C(=O)N2

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity[1].
PBRM1-BD2-IN-8 (0-100 μM; 48 h) inhibits the growth of PBRM1-dependent prostate cancer cells[1].

Reference

[1]. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.
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