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PFI-3

PFI-3

CAS: 1819363-80-8

Molecular Formula: C19H19N3O2

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PFI-3 - Names and Identifiers

Name PFI-3
Synonyms PFI3
PFI-3
PFI 3
CS-1803
(2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-2-propen-1-one
(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
(2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
2-Propen-1-one, 1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-, (2E)-
CAS 1819363-80-8

PFI-3 - Physico-chemical Properties

Molecular FormulaC19H19N3O2
Molar Mass321.37
Solubility Soluble in DMSO (>25 mg/ml)
Appearancepowder
Coloryellow to orange
Storage Condition2-8°C
StabilityStable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
In vitro studyPFI-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.

PFI-3 - Risk and Safety

WGK Germany3

PFI-3 - Preparation solution concentration reference

 1mg5mg10mg
1 mM3.112 ml15.558 ml31.117 ml
5 mM0.622 ml3.112 ml6.223 ml
10 mM0.311 ml1.556 ml3.112 ml
5 mM0.062 ml0.311 ml0.622 ml
Last Update:2024-01-02 23:10:35

PFI-3 - 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)
TargetValue
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
PFI-3
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Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: PFI-3 Visit Supplier Webpage Request for quotation
CAS: 1819363-80-8
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Hubei Rhema Reference Materials Technology Co., Ltd.
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Product Name: PFI3 Request for quotation
CAS: 1819363-80-8
Tel: 0712-8899838
Email: jy6101@rmastandards.com
Mobile: 86-15787876101
QQ: 2518299249 Click to send a QQ message
Wechat: 15787876101
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product 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 Request for quotation
CAS: 1819363-80-8
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product 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 Visit Supplier Webpage Request for quotation
CAS: 1819363-80-8
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: PFI-3 Visit Supplier Webpage Request for quotation
CAS: 1819363-80-8
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
BOC Sciences
Spot supply
Product Name: PFI-3 Visit Supplier Webpage Request for quotation
CAS: 1819363-80-8
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: PFI-3 Visit Supplier Webpage Request for quotation
CAS: 1819363-80-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
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