SML0352

PFI-1

≥98% (HPLC)

• Sinónimos: 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydro-quinazolin-6-yl)-bezenesulfonamide, PF-06405761
• Fórmula empírica (notación de Hill): C₁₆H₁₇N₃O₄S
• Número de CAS: 1403764-72-6
• Peso molecular: 347.39
• Número MDL: MFCD22580416
• Código UNSPSC: 12352202
• ID de la sustancia en PubChem: 329825355
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• color: white to beige
• solubilidad: DMSO: ≥10 mg/mL
• temp. de almacenamiento: 2-8°C
• cadena SMILES: 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)
• Clave InChI: TXZPMHLMPKIUGK-UHFFFAOYSA-N

Descripción

Aplicación

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.

Acciones bioquímicas o fisiológicas

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

Características y beneficios

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.

Otras notas

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.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable