SML0352

PFI-1

≥98% (HPLC)

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

Properties

• 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

Description

Application

PFI-1 has been used as a bromodomain inhibitor in breast cancer cell line MCF7[1] dechorionated zebrafish embryos.[2] It has also been used in human peripheral blood mononuclear cells (PBMCs), to inhibit the release of interleukin-6 in lipopolysaccharide (LPS) challenge assay.[3]

Biochem/physiol Actions

PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells.[4] It elicits minimum toxicity and is effective for anti-HIV-latency therapy.[5] In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.[6]

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

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable