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About This Item
Empirical Formula (Hill Notation):
C16H17N3O4S
CAS Number:
Molecular Weight:
347.39
MDL number:
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: ≥10 mg/mL
storage temp.
2-8°C
SMILES string
COc1ccccc1S(=O)(=O)Nc2ccc3NC(=O)N(C)Cc3c2
InChI
1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)
InChI key
TXZPMHLMPKIUGK-UHFFFAOYSA-N
Application
PFI-1 has been used as a bromodomain inhibitor in breast cancer cell line MCF7 dechorionated zebrafish embryos. It has also been used in human peripheral blood mononuclear cells (PBMCs), to inhibit the release of interleukin-6 in lipopolysaccharide (LPS) challenge assay.
Biochem/physiol Actions
PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells. It elicits minimum toxicity and is effective for anti-HIV-latency therapy. In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.
Selective BET (bromodomain-containing protein) inhibitor.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). For full characterization details, please visit the PFI-1 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-1 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.
Other Notes
PFI-1 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PFI-1 probe summary on the Chemical Probes Portal website.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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