Berberine chloride hydrate is an alkaloid in several plants with various biological functions, including insulin-sensitizing, anti-inflammatory, and anti-oxidant activity. Berberine chloride hydrate is an AMPK activator.
Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator[1]. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.
Ipafricept (OMP-54F28; FZD8-Fc) is the first class of recombinant fusion proteins, consisting of the extracellular portion of the human fried-8 receptor fused to the Fc fragment of human IgG1 binding to the Wnt ligand. Ipafricept shows solid tumor inhibition activity, with well tolerance[1].
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway[1].
Pin1 modulator 1 (compound IIb-219) is a modulator that specifically targets β-Catenin and inhibits the Wnt pathway. Pin1 modulator 1 can be used in the study of Wnt-mediated related diseases, such as cancer[1].
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM[1]. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth[1].
HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction[1].
PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity[1].