Porcupine

LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.

Wnt-C59 (C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

Zamaporvint (RXC004) is a selective, orally active and potent inhibitor of the Wnt pathway that acts on the membrane-bound fatty acyltransferase porcupine to block Wnt ligand palmitoylation, secretion, and pathway activation.Zamaporvint has shown anti-tumor and anti-proliferative activity in a wide range of cancer cell lines.

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM.

IWP L6 (Porcn Inhibitor III) is a highly potent Porcn inhibitor with an EC50 of 0.5 nM.

IWP-O1, a highly potent Porcupine (Porcn) inhibitor (EC50: 80 pM), effectively suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.

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

IWP 12 is a highly efficient Porcupine (Porcn) inhibitor that inhibits the Wnt signaling pathway, blocking tail fin regeneration in both adult and juvenile fish.

Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).

GNF-1331 is a potent, selective, and orally bioavailable porcupine inhibitor (IC50 = 12 nM). Blocking abnormal Wnt signaling is an attractive treatment for a variety of cancers.