porcn

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.

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

Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor with an IC50 of 0.05 nM, applicable in cancer research including sarcoma, melanoma, skin cancer, hematological tumors, lymphoma, carcinoma, and leukemia [1].

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 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.

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.

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].

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

WHN-88, a Porcupine (PORCN) inhibitor, disrupts the palmitoylation of Wnt ligands, which inhibits their secretion and subsequent Wnt β-catenin signaling. This compound has shown efficacy in reducing cancer cell stemness and suppressing the progression and development of breast tumors in MMTV-Wnt1 transgenic mice.