25 products were found matching "K00181"!

Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4...

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to beta-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production...

IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM. IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. At 5 µM, IWP-4 has been shown to...

Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A...

IWP-O1 is an inhibitor of porcupine (PORCN), an enzyme that catalyzes palmitoylation of Wnt proteins. It inhibits Wnt signaling in L-Wnt-STF cells (IC50 = 80 pM in a reporter assay) and phosphorylation of Dishevelled-2 (Dvl2) and Dvl3 in HeLa cells when used at a concentration of 1 µM. IWP-O1 (1 µM) enhances the...

Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM). It suppresses the...

LGK-974 inhibits PORCN, suppressing Wnt signaling. This compound exhibits anticancer chemotherapeutic activity and is currently in clinical trials. LGK-974 inhibits proliferation and induces differentiation of pancreatic adenocarcinoma xenografts, it also shows efficacy in suppressing tumor growth in animal models...

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to beta-catenin activation of gene transcription. IWP-2 (Cay-13951) is an inhibitor of Wnt...

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to beta-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production...

ETC-159 is a potent and orally bioavailable inhibitor of porcupine (PORCN, IC50s = 18.1 and 70 nM for mouse and Xenopus PORCN, respectively). It inhibits beta-catenin reporter activity (IC50 = 2.9 nM) and reduces the interaction of Wnt with its carrier protein WLS via decreased Wnt palmitoleation in STF3A cells, an...

Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.

PORCN is a porcupine homolog protein that belongs to the evolutionary conserved porcupine gene family. Genes of this family encode multi-pass endoplasmic reticulum proteins. Porcupine proteins play an important role in regulating Wnt signaling. Deficiency or mutation in X-linked PORCN causes focal dermal...