For research use only. Not for therapeutic Use.
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[1][2][3][4].
GNF-6231 inhibits Porcupine enzyme activity with IC50 0.8 nM and isn’t cytotoxic in the concentration range of 20 μM[1].
GNF-6231 (5 mg/kg; Intravenous injection (i.v.); every 24 hours for 6 days) alleviates the symptoms of myocardial infarction in C57Bl/6 mice by inhibiting the activation of the Wnt pathway[1].
GNF-6231 (0.3-3 mg/kg; p.o.; once daily for 2 weeks) shows antitumor activity in a mouse of MMTV-WNT1 xenograft tumor[4].
| Catalog Number | I000966 |
| CAS Number | 1243245-18-2 |
| Synonyms | N-[5-(4-acetylpiperazin-1-yl)pyridin-2-yl]-2-[6-(2-fluoropyridin-4-yl)-5-methylpyridin-3-yl]acetamide |
| Molecular Formula | C24H25FN6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H25FN6O2/c1-16-11-18(14-28-24(16)19-5-6-26-21(25)13-19)12-23(33)29-22-4-3-20(15-27-22)31-9-7-30(8-10-31)17(2)32/h3-6,11,13-15H,7-10,12H2,1-2H3,(H,27,29,33) |
| InChIKey | AXXNRMISICMFNS-UHFFFAOYSA-N |
| SMILES | CC1=CC(=CN=C1C2=CC(=NC=C2)F)CC(=O)NC3=NC=C(C=C3)N4CCN(CC4)C(=O)C |
| Reference | [1]. Bastakoty, Dikshya et al. Temporary, Systemic Inhibition of the WNT/β-Catenin Pathway promotes Regenerative Cardiac Repair following Myocardial Infarct. Cell, stem cells and regenerative medicine vol. 2,2 (2016): 10.16966/2472-6990.111. [2]. Kang, Sheng. Low-density lipoprotein receptor-related protein 6-mediated signaling pathways and associated cardiovascular diseases: diagnostic and therapeutic opportunities. Human genetics vol. 139,4 (2020): 447-459. [3]. Raeisi, Mortaza et al. Porcn as a novel therapeutic target in cancer therapy: A review. Cell biology international vol. 46,12 (2022): 1979-1991. [4]. Cheng, Dai et al. Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors. ACS medicinal chemistry letters vol. 7,7 676-80. 10 May. 2016, |
