Wnt/beta-catenin

Specnuezhenide (Nuezhenide) significantly protects human neuroblastoma SH-SY5Y cells from 6-hydroxydopamine-induced neurotoxicity.Nuezhenide is the main inhibitory compound of fruits, it shows a clear inhibitory effect to the seeds of wheat and Chinese cabbage.

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.

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

Echinacoside is a natural polyphenolic compound with various kinds of pharmacological activities, such as anti-inflammatory, antioxidative, hepatoprotective, neuroprotective, nitric oxide radical-scavenging and vasodilative ones.

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].

Urea (Carbonyldiamide) is formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end metabolite of protein catabolism and accounts for about one-half of the total urinary solids.

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.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

F7H is a potent Frizzled receptor FZD7 antagonist with an IC50 value of 1.25 μM.F7H is a potent ligand for the transmembrane structural domain (TMD) of FZD7, with potential antitumor and bacteriostatic activity.

Foxy-5 Ammonium Salt is a WNT5A agonist, a mimetic peptide of WNT5A, a non-classical member of the Wnt family.Foxy-5 Ammonium Salt triggers cytoplasmic free calcium signaling without affecting β-catenin activation and inhibits migration and invasion of epithelial cancer cells.Foxy-5 Foxy-5 Ammonium Salt effectively reduces the metastatic spread of prostate cancer cells with low WNT5A expression in an in situ mouse model.

PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has potential anti-tumor activity and induces apoptosis.

ICG001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

TNIK-IN-7 is a potent and selective Traf2 and Nck interacting kinase (TNIK) inhibitor (IC50: 11 nM) with antitumor activity for studying signaling and proliferation in colorectal cancer cells.

TNKS-2-IN-2 is a novel and potent TNKS2 selective inhibitor (IC50: 22 nM) with potential anti-tumour activity for the study of colon cancer lung cancer and breast cancer.

YW2036 is an inhibitor of Wnt signaling pathway.

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.

Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch/Wnt signaling and induces apoptosis.

β-catenin modulator IIa-661 is a small molecule inhibitor of the Wnt pathway with antitumour activity.

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.

NRX-103094 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, which enhances the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

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

DK419 is an orally active inhibitor of Wnt/β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK.

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.

Miclxin (DS37262926) is a novel MIC60 inhibitor that induces apoptosis through mitochondrial stress in mutant tumor cells via β-catenin.Miclxin is a potent inhibitor of mutant β-catenin, which is involved in the Wnt signaling pathway.Miclxin induces β-catenin-dependent apoptosis, leading to mitochondrial damage and loss of mitochondrial membrane. Miclxin has anti-tumor activity and kills tumors by targeting MIC60.

Carboxylesterase-IN-3 is a potent inhibitor of Carboxylesterase Notum (IC50 ≤ 10 nM).Carboxylesterase-IN-3 has the potential to study cancer diseases.

SRI 37892 is a Fzd7 inhibitor with potent activities against Wnt/β-catenin signaling and cancer cell viability.

NRX-103095 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and enhances the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 163 nM.

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein protein interaction ( β catenin/BCL9 PPI ) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a K i value of 0.76 μM and an IC 50 value of 0.87 μM [1]. ZW4864 (free base) shows good pharmacokinetic properties.

NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation(EC50：3.8 nM)

NRX-252114 (NRX252114) induces degradation of mutant β-catenin NRX-252114 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, and is able to enhance the binding of pSer33/S37A β-catenin to β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. Kd is 0.4 nM.

TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].

CCT 031374 hydrobromide is a TCF/β-catenin inhibitor with antitumor activities.

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11/4 nM). XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription.

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 (IC50 < 2 μM)

Wnt-C59 (C59)(C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.

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

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

WAY262611 is a Wnt/β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay.

IWR-1 (IWR-1-endo), a Wnt pathway inhibitor, stabilizes the Axin destruction complex(EC50=0.2 uM).

Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.

WIC1 is a potent Wnt inhibitor. WIC1 can be used in cancer research

TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.

(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell

Wnt pathway inhibitor 3 is a potent AC1 inhibitor with an IC50 value of 45 nM.Wnt pathway inhibitor 3 has antiproliferative activity and can be used in studies to ameliorate osteoarthritis in a mouse model of experimental osteoarthritis.

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant

IWP-O1 is a highly potent Porcupine (Porcn) inhibitor (EC50: 80 pM), effectively suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.

TINK-IN-1 is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

FIDAS-3, a stilbene derivative and potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A), exhibits anticancer activities by effectively competing with S-adenosylmethionine (SAM) for MAT2A binding.

Teplinovivint is a potent inhibitor of the Wnt/β-catenin signaling pathway, demonstrating anti-inflammatory properties with potential utility in tendinopathy research.