For research use only. Not for therapeutic Use.
PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer[1].
PBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides[1].
| Catalog Number | I042610 |
| CAS Number | 2819989-61-0 |
| Synonyms | 5-chloro-2-(3-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one |
| Molecular Formula | C15H13ClN2O |
| Purity | ≥95% |
| InChI | InChI=1S/C15H13ClN2O/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 | OBDBCXGMLSMARG-UHFFFAOYSA-N |
| SMILES | CC1=CC(=CC=C1)C2NC3=C(C(=CC=C3)Cl)C(=O)N2 |
| Reference | [1]. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13. |
