SML0939
PFI-3
≥98% (HPLC)
Synonym(s):
(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
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About This Item
Empirical Formula (Hill Notation):
C19H19N3O2
CAS Number:
Molecular Weight:
321.37
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
Product Name
PFI-3, ≥98% (HPLC)
SMILES string
OC1=C(C(/C=C/N2[C@H](C3)CN(C4=NC=CC=C4)[C@H]3C2)=O)C=CC=C1
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
InChI key
INAICWLVUAKEPB-QSTFCLMHSA-N
assay
≥98% (HPLC)
form
powder
color
yellow to orange
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
Related Categories
Biochem/physiol Actions
PFI-3 is a SCG probe for SMARCA 2 and SMARCA 4, members of the large ATP-dependent chromatin remodeling complex SNF/SWI.
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
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
Features and Benefits
PFI-3 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Seul Gi Park et al.
Scientific reports, 10(1), 16330-16330 (2020-10-03)
Bromodomain (BRD), a protein module that recognizes acetylated lysine residues on histones and other proteins, has recently emerged as a promising therapeutic target for human diseases such as cancer. While most of the studies have been focused on inhibitors against
Chromatin Remodeling Factor BRG1 Regulates Stemness and Chemosensitivity of Glioma Initiating Cells.
Debolina Ganguly et al.
Stem cells (Dayton, Ohio), 36(12), 1804-1815 (2018-09-02)
Glioblastoma multiforme (GBM) is a highly aggressive and malignant brain tumor that is refractory to existing therapeutic regimens, which reflects the presence of stem-like cells, termed glioma-initiating cells (GICs). The complex interactions between different signaling pathways and epigenetic regulation of
Jin Wei et al.
Cell, 184(1), 76-91 (2020-11-05)
Identification of host genes essential for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection may reveal novel therapeutic targets and inform our understanding of coronavirus disease 2019 (COVID-19) pathogenesis. Here we performed genome-wide CRISPR screens in Vero-E6 cells with SARS-CoV-2
Julia Minderjahn et al.
Nature communications, 11(1), 402-402 (2020-01-23)
Establishing gene regulatory networks during differentiation or reprogramming requires master or pioneer transcription factors (TFs) such as PU.1, a prototype master TF of hematopoietic lineage differentiation. To systematically determine molecular features that control its activity, here we analyze DNA-binding in
Irena Hlushchuk et al.
ACS chemical neuroscience, 12(13), 2273-2279 (2021-06-11)
Neurodegenerative diseases are associated with failed proteostasis and accumulation of insoluble protein aggregates that compromise neuronal function and survival. In Parkinson's disease, a major pathological finding is Lewy bodies and neurites that are mainly composed of phosphorylated and aggregated α-synuclein
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