porcupine

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

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

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

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.

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

IWP-3 is a potent inhibitor of Wnt production with an IC50 of 40 nM. It inhibits Porcupine (Porcn), blocking the palmitoylation of Wnt proteins, and moderately inhibits CK1γ3 and CK1ε, but does not inhibit CK1α [1] [2].

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

Potent inhibitor of Porcupine (PORCN)

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.

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.