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Description

A cell-permeable pyridinylphenyl-acetamide that is much more potent than IWP-2 (Cat. No. 681671) in inhibiting MBOAT family member Porcupine-mediated Wnt palmitoylation (IC50 = 74 pM in STF reporter assays using Wnt3a-transfected HEK293). Shown to be effective against Porcn of murine and human, but not xenopus, species and potently inhibit the processing of both canonical and non-canonical 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.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., 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 orally active in mice (t1/2 = 1.94 h, plasma [C59]t = 24 h = 3 nM, 5 mg/mL p.o.) and demonstrated to effectively suppress MMTV-WNT1 tumor expansion in both immunodeficient female nude mice (Ave fold of tumor expansion = 3 vs.19 in 17 days with or without daily 10 mg/kg oral dosage) and in immunocompetent female nulliparous mice (Ave fold of tumor expansion = 0.8 vs.3.7 in 21 days with or without daily 5 mg/kg oral dosage) in vivo.