wnt pathway

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

Wnt pathway activator 2, with an IC50 of 13 nM, is a potent Wnt activator.

Wnt pathway activator 1 is a potent Wnt activator with an IC50 of 28-29 nM. Wnt pathway activator 1 is a potent Wnt activator for the treatment of androgenetic alopecia (AGA).

Wnt pathway inhibitor 4 is a small molecule antimicrobial agent with antibacterial and antiproliferative activity against cancer cells.

Wntpathway inhibitor 5 (Compound 28) is an effective wntpathway inhibitor with an IC50 value of less than 0.003 μM. This compound can suppress various types of cancers such as ovarian teratoma, breast cancer, osteosarcoma, and head and neck squamous cell carcinoma.

Wnt pathway inhibitor 3 is a potent AC1 inhibitor (IC50: 45 nM) with antiproliferative activity, suitable for studies to ameliorate osteoarthritis in a mouse model of experimental osteoarthritis.

YB-0158 ammonium (Wnt pathway inhibitor 2 ammonium) is a reverse-rotation peptidomimetic small molecule with translation-enhancing potential and anticancer activity. YB-0158 ammonium disrupts Sam68-Src interaction and induces apoptosis in colorectal cancer cells, which can be used to study cancer.

BML-286 is a WNT pathway modulator with potential anticancer activity, inducing β-catenin- and TCF-dependent transcriptional activity, and can be used in the study of degenerative diseases, intestinal, breast, bladder, gastric, melanoma, leukemia, hepatocellular carcinoma and nephroblastoma.

YB-0158 (Wnt pathway inhibitor 2) is a potent peptidomimetic compound that targets colorectal cancer stem cells (CSCs) by disrupting the interaction between Sam68 and Src proteins. As a reverse-turn agent, it induces apoptosis in CRC cells and exhibits strong anti-cancer activity.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

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.

Adavivint (SM04690) is a selective inhibitor of the typical Wnt signaling pathway. In SW480 cells, EC50=19.5 nM was measured using high-throughput TCF/LEF reporter gene experiments.

SKL2001, an agonist of the Wnt/β-catenin pathway, can disrupt the Axin/β-catenin interaction.

Vantictumab (OMP-18R5) is a humanized anti-FZD1/2/5/7/8 monoclonal antibody that inhibits Wnt pathway signaling and is used in research studies for the treatment of metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt/β-catenin pathway.

NKP608 is a selective and highly effective neurokinin-1 (NK-1) receptor antagonist with anticancer and antianxiety activities, inhibiting the proliferation of human colorectal cancer cells through the Wnt signaling pathway.

Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway, and increases apoptosis in lung cancer cells. Hematein is an oxidation product of hematoxylin acted as a dye and it also is an allosteric casein kinase II inhibitor (IC50: 0.74 μM).

Methyl vanillate is Hovenia Dulcis Thunb extract and its ingredient methyl vanillate activate Wnt/β-catenin pathway and increase bone mass in growing or ovariectomized mice. Methyl vanillate is considered to be a slightly soluble (in water) acidic compound. Methyl vanillate can be synthesized from vanillic acid. Methyl vanillate has been identified in foods such as cow's milk and beer.

1. Isoquercetin (3-Glucosylquercetin) is a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders. 2. Isoquercetin may be as a potential therapeutic agent against neurodegeneration in Parkinson's disease. 3. Isoquercetin is an inhibitor of Wnt/β-catenin and may be as a potential novel anti-tumoral agent, such as against human pancreati,liver cancer related to opioid receptors and to the activation of the mitogen-activated protein kinase (MAPK) signalling pathway. .

Pyrvinium pamoate (Pyrvinium embonate) is an old anthelminthic medicine for the treatment of enterobiasis , which re-attracts attention as an anti-cancer drug due to its inhibition of Wnt/β-catenin pathway in some types of cancer.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].