5.00496

C59

≥99% (HPLC), powder, Porcn inhibitor, Calbiochem^®

• Synonym(e): Porcn Inhibitor II, C59, NAN, Wnt-C59, Wnt Pathway Inhibitor XVI, 2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
• Empirische Formel (Hill-System): C₂₅H₂₁N₃O
• CAS-Nummer: 1243243-89-1
• Molekulargewicht: 379.45
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• product name: Porcn Inhibitor II, C59,
• Assay: ≥99% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C
• InChI: 1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29)
• InChIKey: KHZOJCQBHJUJFY-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

A cell-permeable pyridinylphenyl-acetamide that is much more potent than IWP-2 (Cat. No. 681671) in inhibiting MBOAT (membrane-bound O-acyltranferase) family member Porcn- (Porcupine) mediated Wnt palmitoylation (IC50 = 74 pM in STF reporter assays using Wnt3a-transfected HEK293 cells). Shown to be effective against Porcn of murine (mPorcn-A, B, C, D) and human (hPorcn-B), but not xenopus (xPorcn-A), species and potently inhibit the processing of both canonical (1, 2, 3a, 6, 7b, 8a, 9a, 9b, 10) and non-canonical (4, 5a, 11, 16) Wnt subtypes. C59 is demonstrated to be orally active and effectively suppress MMTV-WNT1 tumor expansion in mice (5 mg/kg & 10 mg/kg p.o.) in vivo.

Anwendung

Porcn Inhibitor II, C59 has been used as a Wnt inhibitor in the differentiation protocol of hiPSCs to cardiomyocytes.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Porcupine (Porcn)-mediated Wnt palmitoylation

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sonstige Hinweise

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable