PFI 4
PFI 4 is a cell permeable, potent and selective inhibitor of BRPF1 Bromodomain with pIC50 and pKd values of 7.1 and 8.0 [1].
The BRPF (bromodomain and PHD finger-containing) family BRPF1, BRPF2/BRD1, and BRPF3 operate as scaffolds to assemble MYST-family histone acetyltransferases (HATs) complexes. BRPF1 is a component of complexes containing the MOZ/MORF transcriptional coactivators and links the catalytic HATs to the other subunits ING5 and hEAF6.8. BRPF1 is important for maintaining skeletal development and Hox gene expression in fish [1].
In the BROMOscan panel of 35 bromodomain binding assays, PFI 4 exhibited excellent BRPF1 potency with pKd value of 8.0 and excellent selectivity over other bromodomains. In a cellular protein interaction assay, PFI 4 displaced NanoLuc-tagged BRPF1 bromodomain from Halotagged
histone H3.3 and disrupted chromatin binding [1].
Reference:
[1]. Demont EH, Bamborough P, Chung CW, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett, 2014, 5(11): 1190-1195.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 380.44 |
| Cas No. | 900305-37-5 |
| Formula | C21H24N4O3 |
| Solubility | insoluble in H2O; ≥13.3 mg/mL in DMSO; ≥2.87 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N-(1,3-dimethyl-2-oxo-6-(pyrrolidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide |
| SDF | Download SDF |
| Canonical SMILES | [H]N(C(C1=CC=CC=C1OC)=O)C2=C(N3CCCC3)C=C(N(C)C(N4C)=O)C4=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
Chemical structure
