β-catenin Agonist

SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.

WAY-262611 is a Wnt/β-Catenin agonist that increases bone formation rate with an EC₅₀ of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.

Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.

QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC₅₀ of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.

FzM1.8, derives from FzM1, is an allosteric agonist of FZD4 with pEC₅₀ of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.

Wnt/β-catenin agonist 2 is a potent Wnt agonist. Wnt/β-catenin agonist 2 activates Wnt/β-catenin signaling and can be used in the research of diseases related to the signal transduction. (From patent WO2007078113A1, compound 39)

N-Acetylgalactosaminyltransferase 1 (GALNT1) is a glycosyltransferase that initiates mucin-type O-glycosylation by transferring α-GalNAc from UDP-GalNAc to serine (Ser) or threonine (Thr) residues in proteins. Overexpression of N-Acetylgalactosaminyltransferase 1 in gastric cancer can promote abnormal O-glycosylation of CD44, thereby activating the Wnt/β-catenin signaling pathway and regulating the malignant behavior of gastric cancer cells. Additionally, N-Acetylgalactosaminyltransferase 1 plays a crucial role in cancer growth and metastasis by modifying the O-glycosylation of various glycoproteins, such as mucin (MUC1), osteopontin (OPN), matrix metalloproteinase-14 (MMP14), and integrin α3.

Wnt/β-catenin agonist 3 (compound 98) is a Wnt/β-catenin signalling pathway agonist. Wnt/β-catenin agonist 3 can be used for the research of osteoporosis.

BMP agonist 1 (compound 2 b) is a small-molecule agonist of bone morphogenic protein (BMP). BMP induces C2C12 cell differentiation with BMP and highly depends on active BMP signaling. BMP agonist 1 inhibits GSK3β, increases β-catenin signaling and synergistically regulates Id2and Id3 expression. BMP agonist 1 is used in diseases and defects of the skeleton research.

SLD1121 is an agonist of the Wnt/β-catenin signaling pathway that enhances Wnt signaling by targeting LRP6 (K_d: 4.52-7.49 nM). SLD1121 interacts with the intracellular domain of LRP6, stabilizes LRP6, promotes its nuclear translocation, and facilitates its binding to β-catenin, TCF4 or LEF1 in the nucleus, thereby inducing the expression of Wnt-regulated genes and stem cell-related genes. SLD1121 induces the transition of hair follicles from telogen to anagen in the mouse hair growth cycle and promotes hair growth in mice. SLD1121 is applicable to hair loss-related research.

SKL2001 (GMP) is SKL2001 (HY-101085) produced by using GMP guidelines. SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.

SKL2001 (Standard) is the analytical standard of SKL2001 (HY-101085). This product is intended for research and analytical applications. SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.