PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
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.
Salinomycin is an anticoccidial drug with potent anti-bacterial activity and an novel anticancer agent targeting human cancer stem cells.
FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
XAV-939 is a tankyrase (TNKS) inhibitor and an indirect inhibitor of Wnt/β-catenin signaling, with IC50s of 5 and 2 nM for TNKS1 and TNKS2, respectively.
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity.
Triptonide(NSC 165677; PG 492), extracted from Tripterygium wilfordii Hook, inhibited the proliferation of mouse splenocytes induced by suboptimal concentration of concanavalin A or lipopolysaccharide at concentrations of 0.02, 0.1, and 0.5 mg/ml.
Berberine has shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells; MAPK and Wnt/β-catenin pathways affected by Berberine.IC50 value:Target: Anticancer agentThe plant-based alkaloid berberine has potential therapeutic applications for breast cancer, although a better understanding of the genes and cellular pathways regulated by this compound is needed to define the mechanism of its action in cancer treatment. In this review, the molecular targets of berberine in various cancers, particularly breast cancer, are discussed. Berberine was shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells. Some signaling pathways affected by berberine, including the MAP (mitogen-activated protein) kinase and Wnt/β-catenin pathways, are critical for reducing cellular migration and sensitivity to various growth factors [1]. Treatment with BBR(Berberine) in rats on the atherogenic diet reduced plasma total cholesterol and nonHDL cholesterol levels by 29%-33% and 31%-41%, respectively, with no significant differences being observed among the three doses [2]. Berberine induced both apoptotic and autophagic death of HepG2 cells, which was associated with a significant activation of AMPK and an increased expression of the inactive form of acetyl-CoA carboxylase (ACC) [3]. Berberine did not show major effects on viability of HEK-293 embryonic kidney and HCT116 colon carcinoma cells and was not toxic in concentrations up to 20 μM. Berberine inhibited β-catenin transcriptional activity and attenuated anchorage-independent growth. As a result of berberine treatment, cellular levels of active β-catenin were reduced concomitant with an increase in the expression of E-cadherin [4].
KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
Cardiogenol C hydrochloride is a cell-permeable pyrimidine compound which potently induces the differentiation of ESCs into cardiomyocytes (EC50= 100 nM).IC50 value: 100 nM (EC50)Target:in vitro: Cardiogenol C hydrochloride is a cardiomyogenesis inducer in embryonic stem cells. Cardiogenol C induces the differentiation of myosin heavy chain-positive cardiomyocytes from embryonic stem cells with an EC50 value of 0.1 μM; about 90% of embryonic stem cells treated with 0.25 μM of Cardiogenol C express the cardiac muscle cell specific transcription factors GATA-4, MEF2, and Nkx2.5 and display the characteristic beating behavior of differentiated cardiomyocytes. Cardiogenol C (a diaminopyrimidine) induces cardiac differentiation in P19 and in P19Cl6 cells. [1] Cardiogenol C could activate Wnt/β-catenin signaling to induce cardiogenesis. Cardiogenol C-treatment significantly decreased HBPCs proliferation. Cardiogenol C was able to induce HBPCs to transdifferentiate into cardiomyocyte-like cells.[2]
Pamidronic acid is a drug used to treat a broad spectrum of bone absorption diseases.
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay.
WIKI4 is a potent inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM).
Nefopam is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain.