For research use only. Not for therapeutic Use.
PFI-3（Cat No.:I005862）is a selective small molecule inhibitor that targets BRD4 (bromodomain-containing protein 4), a member of the BET (bromodomain and extraterminal) family of proteins. BRD4 plays a crucial role in regulating gene expression by interacting with acetylated histones, and it is involved in cancer cell growth, survival, and metastasis. By inhibiting BRD4, PFI-3 aims to block these oncogenic pathways and reduce tumor progression. It has shown potential in preclinical studies, particularly in hematological cancers like leukemia and lymphoma, as well as in solid tumors. Further clinical development is needed to assess its therapeutic potential and safety.
| Catalog Number | I005862 |
| CAS Number | 1819363-80-8 |
| Molecular Formula | C19H19N3O2 |
| Purity | ≥95% |
| Target | PBRM1/SMARCA4 |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| Storage | Store at -20°C |
| IC50 | 48 nM/89 nM(PBRM1/SMARCA4) |
| IUPAC Name | (E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one |
| InChI | InChI=1S/C19H19N3O2/c23-17-6-2-1-5-16(17)18(24)8-10-21-12-15-11-14(21)13-22(15)19-7-3-4-9-20-19/h1-10,14-15,23H,11-13H2/b10-8+/t14-,15-/m1/s1 |
| InChIKey | INAICWLVUAKEPB-QSTFCLMHSA-N |
| SMILES | C1[C@@H]2CN([C@H]1CN2C3=CC=CC=N3)/C=C/C(=O)C4=CC=CC=C4O |
| Reference | [1]The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.<br /> |
