PFI3
- Product Name
- PFI3
- CAS No.
- 1819363-80-8
- Chemical Name
- PFI3
- Synonyms
- PFI3;PFI-3;CS-1803;PFI3; PFI 3;PFI3 USP/EP/BP;Inhibitor,Epigenetic Reader Domain,PFI3,PFI-3,inhibit;(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)-
- CBNumber
- CB62729372
- Molecular Formula
- C19H19N3O2
- Formula Weight
- 321.37
- MOL File
- 1819363-80-8.mol
PFI3 Property
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (>25 mg/ml)
- form
- powder
- color
- yellow to orange
- Stability:
- Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0939
- Product name
- PFI-3
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $113
- Updated
- 2023/06/20
- Product number
- SML0939
- Product name
- PFI-3
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $453
- Updated
- 2023/06/20
- Product number
- 15267
- Product name
- PFI-3
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 15267
- Product name
- PFI-3
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 15267
- Product name
- PFI-3
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
PFI3 Chemical Properties,Usage,Production
Description
PFI-3 (1819363-80-8) is a selective inhibitor of family VIII bromodomains PB1(5), SMARCA2, and SMARCA4.1 It showed complete selectivity over all non-family VIII bromodomains.? PFI-3 blocked adipogenesis in C3H10T1/2 mesenchymal cells at 20μM.Treatment of embryonic stem cells with PFI-3 led to deprivation of stemness and deregulated lineage specificity. Differentiation of trophoblast stem cells in the presence of PFI-3 was enhanced.2 Cell permeable.
Uses
PFI-3 is a selective chemical inhibitor for SMARCA (2/4) and PBI (5) bromodomains which may result in the delay and prevention of breast cancer.
Definition
ChEBI: PFI-3 is an azabicycloalkane that is (1R,4R)-2,5-diazabicyclo[2.2.1]heptane which is substituted at position 2 by a 3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl group and at position 5 by a pyridin-2-yl group. It is a potent and selective inhibitor of polybromo 1 (Kd = 48 nM), SMARCA2 and SMARCA4 (Kd = 89 nM) bromodomains. It is a member of pyridines, an azabicycloalkane, a member of phenols and an enone.
Biochem/physiol Actions
SMARCA4 (SWI/SNF related, Matrix associated, Actin dependent Regulator of Chromatin, subfamily A, member 4) is a transcriptional activator and is a component of the large ATP-dependent chromatin remodeling complex SWI/SNF, which is required for transcriptional activation of genes normally repressed by chromatin. SMARC4 (also known as BRG1) and the related protein SMARCA2 (also known as BRM) contain a bromodomain that is structurally similar to the PolyBromo1 (PB1) 5 bromodomain. PFI-3 is a selective chemical probe for SMARCA bromodomains that inhibits SMARCA2, SMARCA4 and PB1(5) bromodomains. For full characterization details, please visit the PFI-3 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
storage
Store at -20°C
References
Gerstenberger et al. (2016), Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit; J. Med. Chem. 59 4800 Fedorov et al. (2015), Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance; Sci. Adv. 1 e1500723
PFI3 Preparation Products And Raw materials
Raw materials
Preparation Products
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