2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)-
PFI-3
CAS: 1819363-80-8
Molecular Formula: C19H19N3O2
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)- - Names and Identifiers
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)- - Physico-chemical Properties
| Molecular Formula | C19H19N3O2 |
| Molar Mass | 321.37 |
| Solubility | Soluble in DMSO (>25 mg/ml) |
| Appearance | powder |
| Color | yellow to orange |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| In vitro study | PFI-3 selectivity for PB1(5) and SMARCA2/4 was significantly higher than the 36 other kinases tested. PFI-3 was significantly more selective for PB1(5) and SMARCA2/4 than the 36 other kinases tested. PFI-3 is a potent, cell-active inhibitor of protein interactions that selectively binds to the basic BAF bromine region. In a screening experiment with 102 cell receptors and 30 enzymes, PFI-3 had micromolar affinity for only four GPCRs and no interaction with proteins outside the BRD family, it shows that PFI-3 has good drug selectivity. Stability testing demonstrated that the half-life of PFI3 in liquid solutions was more than 7 days at 37 °c. In long-term experiments, PFI-3 were able to significantly alter gene expression programs critical to stem cell differentiation. PFI-3 can mimic the effect of Brg1 deletion, causing an increase in the inhibitory H3K27me3 marker, Gene Stat3 binding site, in TSSs. PFI-3 in 20 C, pH7.4 PBS, the half-life of more than 250 h. |
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)- - Risk and Safety
| WGK Germany | 3 |
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.112 ml | 15.558 ml | 31.117 ml |
| 5 mM | 0.622 ml | 3.112 ml | 6.223 ml |
| 10 mM | 0.311 ml | 1.556 ml | 3.112 ml |
| 5 mM | 0.062 ml | 0.311 ml | 0.622 ml |
Last Update：2024-01-02 23:10:35
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)- - Reference Information
| biological activity | PFI-3 is a SMARCA-bromodomains selective chemical probe, including SMARCA2, SMARCA4 and PB1(5) bromodomains. PFI-3 is a SMARCA-bromodomains selective chemical probe, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
| in vitro study | the selectivity of PFI-3 to PB1(5) and SMARCA2/4 was significantly higher than that of 36 other tested kinases. the selectivity of PFI-3 to PB1(5) and SMARCA2/4 was significantly higher than that of 36 other tested kinases. PFI-3 is an effective and cell-active protein interaction inhibitor that can selectively bind to the basic BAF bromine region. In the screening experiment with 102 kinds of cell receptors and 30 kinds of enzymes, PFI-3 has only micro-molar affinity for four GPCRs and has no interaction with proteins outside BRD family, indicating that PFI-3 has good drug selectivity. The stability test proved that PFI3 had a half-life of more than 7 days in liquid solution at 37°C. In long-term experiments, PFI-3 can significantly change the gene expression program that is essential for stem cell differentiation. PFI-3 can simulate the effect of Brg1 deletion and cause the increase of inhibitory H3K27me3 markers and Stat3 binding sites in TSSs. PFI-3 in PBS at 20 ℃ and pH7.4, the half-life is more than 250 h. |
| target | TargetValue PB1(5) bromodomains SMARCA4 55 nM (kd) SMARCA2B 72 nM (kd) SMARCA2A 110 nM (kd) |
| Target | Value |
| PB1(5) bromodomains | |
| SMARCA4 (Cell-free assay) | 55 nM(Kd) |
| SMARCA2B (Cell-free assay) | 72 nM(Kd) |
| SMARCA2A (Cell-free assay) | 110 nM(Kd) |
Last Update：2024-04-09 21:04:16
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Spot supply
Product Name: PFI-3 Visit Supplier Webpage Request for quotationCAS: 1819363-80-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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