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SML0352

Sigma-Aldrich

PFI-1

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C16H17N3O4S
CAS Number:
1403764-72-6
Molecular Weight:
347.39
MDL number:
MFCD22580416
UNSPSC Code:
12352202
PubChem Substance ID:
329825355
NACRES:
NA.77

Quality Level

100

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

Related Categories

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.
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.
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.

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wgk_germany

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flash_point_f

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flash_point_c

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Certificates of Analysis (COA)

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PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains
Picaud S, et al.
Cancer Research, 73(11), 3336-3346 (2013)
Estrogen-dependent control and cell-to-cell variability of transcriptional bursting
Fritzsch C, et al.
Molecular Systems Biology, 14(2) (2018)
The BET-inhibitor PFI-1 diminishes AR/AR-V7 signaling in prostate cancer cells
Hupe MC, et al.
World Journal of Urology, 37(2), 343-349 (2019)
Marie C Hupe et al.
World journal of urology, 37(2), 343-349 (2018-06-24)
The bromodomain and extra-terminal (BET) family of proteins provides a scaffolding platform for the recruitment and tethering of transcription factors to acetylated chromatin, thereby modulating gene expression. In this study, we evaluated the efficacy of the BET-inhibitor PFI-1 to diminish
BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency
Lu P, et al.
Scientific reports, 7(1), 16646-16646 (2017)
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