PFI 3
PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4 with Kd values of 48 and 89 nM, respectively [1].
Transcription activator BRG1 (SMARCA4) is a member of the SWI/SNF family and regulates transcription. Protein polybromo-1 (PB1, PBRM1) is a BRG1-associated factor and tumor suppressor.
PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4. PFI 3 bound to SMARCA2 and SMARCA4 bromodomains with Kd values of 55 and 110 nM, respectively. PFI-3 (2 μM) inhibited PBRM1 by 70%. In cell-based chromatin binding assays, PFI-3 replaced GFP-tagged SMARCA2 bromodomain in a dose-dependent way with IC50 value of 5.78 μM. PFI-3 was a cell-permeable probe suitable for studying SMARCA2/4 bromodomains. In the SMARCA4-deficient A549, H1299, H157 cell lines, PFI-3 had no anti-proliferative effects and was unable to replace SMARCA2 from chromatin. In THP-1 and MV4-11 leukemic cells, PFI 3 did not induce anti-cancer phenotype [1].
Reference:
[1]. Vangamudi B, Paul TA, Shah PK, et al. 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. Cancer Res, 2015, pii: canres.3798.2015.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 321.37 |
| Cas No. | 1819363-80-8 |
| Formula | C19H19N3O2 |
| Solubility | insoluble in H2O; ≥15.15 mg/mL in DMSO; ≥2.97 mg/mL in EtOH with ultrasonic |
| SDF | Download SDF |
| Canonical SMILES | O=C(C1=CC=CC=C1O)/C=C/N(C2)[C@@H]3C[C@H]2N(C4=NC=CC=C4)C3 |
| 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
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Chemical structure
