GNF-6231

Research use only, not for human use.

GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.

GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.

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Animal Model:C57Bl/6 mice model of myocardial infarctionDosage:5 mg/kg Administration:Intravenous injection (i.v.); Starting from 6 hours after myocardial infarction surgery to the sixth day after infarction, once every 24 hours Result:Reduced nuclear and cytoplasmic β-catenin levels.Reduced adverse cardiac remodeling and reduced myocardial infarction area in mice (9.07%).Enhanced the overall heart repair and recovery after left ventricular infarction.Animal Model:Mouse MMTV-WNT1 xenograft tumor model Dosage:0.3 mg/kg,1.0 mg/kg, 3 mg/kg Administration:Oral gavage; Once daily for 2 weeks Result:At a single dose of 3 mg/kg, reduced the level of Wnt target gene Axin2 mRNA.Promoted tumor regression in mice in a dose-dependent manner.

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Wnt/Notch/Hedgehog

Porcupine

Porcupine

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1243245-18-2

448.49

C24H25FN6O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 36 mg/mL (80.27 mM )

CC(=O)N1CCN(CC1)c1ccc(NC(=O)Cc2cnc(c(C)c2)-c2ccnc(F)c2)nc1

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(-20℃)

With Ice Pack

≥ 2 years