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PFI-1

SIGMA/SML0352 - ≥98% (HPLC)

Synonym: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydro-quinazolin-6-yl)-bezenesulfonamide; PF-06405761

CAS Number: 1403764-72-6
Empirical Formula (Hill Notation): C16H17N3O4S
Molecular Weight: 347.39
MDL Number: MFCD22580416
Linear Formula: C16H17N3O4S
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML0352-5MG 5 mg
 $125.00
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45-SML0352-25MG 25 mg
 $343.00
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assay ≥98% (HPLC)
color white to beige
form powder
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
Quality Level 100 
SMILES string COc1ccccc1S(=O)(=O)Nc2ccc3NC(=O)N(C)Cc3c2
solubility DMSO: ≥10 mg/mL
storage temp. 2-8°C
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.
Biochem/physiol Actions: Selective BET (bromodomain-containing protein) inhibitor.
Biochem/physiol Actions: 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 
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 .
Features and Benefits: 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.
Packaging: 5, 25 mg in glass bottle
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352202

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