P4359

Pifithrin-α

≥95% (HPLC), powder

• Synonym(e): 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone hydrobromide, PFT-α
• Lineare Formel: C₁₆H₁₈N₂OS·HBr
• CAS-Nummer: 63208-82-2
• Molekulargewicht: 367.30
• MDL-Nummer: MFCD00417851
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 24898529
• NACRES: NA.77

Eigenschaften

• Assay: ≥95% (HPLC)
• Form: powder
• Lagerbedingungen: protect from light
• Farbe: off-white
• mp (Schmelzpunkt): 192.1-192.5 °C (lit.)
• Löslichkeit: DMSO: 20 mg/mL
• Versandbedingung: wet ice
• Lagertemp.: −20°C
• SMILES String: Br[H].Cc1ccc(cc1)C(=O)CN2C(=N)SC3=C2CCCC3
• InChI: 1S/C16H18N2OS.BrH/c1-11-6-8-12(9-7-11)14(19)10-18-13-4-2-3-5-15(13)20-16(18)17;/h6-9,17H,2-5,10H2,1H3;1H
• InChIKey: HAGVCKULCLQGRF-UHFFFAOYSA-N

Beschreibung

Anwendung

Pifithrin-α has been used:

• to study the effect of specific p53 inhibitor on p53-upregulated modulator of apoptosis (PUMA) expression after transient global cerebral ischemia (tGCI)
• as p53 inhibitor to treat PA1 cells
• as a tumor protein p53 (TRP53) inhibitor, to treat mouse lung epithelial-12 (MLE-12) cells

Biochem./physiol. Wirkung

Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Pifithrin-α enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation without an increase in cancer incidence. The protective effect is not seen in p53-null mice or cells expressing a dominant negative mutant of the p53 gene. Protection is conferred by the transient expression of p53 in p53-deficient cell lines.

Leistungsmerkmale und Vorteile

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Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• Persönliche Schutzausrüstung: Eyeshields, Gloves, type N95 (US)