Sempervirine is an alkaloid derived from Gelsemium elegans Benth.. Sempervirine inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces apoptosis by regulating Wnt/β-catenin pathway[1].
Wnt/β-catenin agonist 1 (compound 3f) is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM[1].
Porcn-IN-2 (Example 107) is a Wnt inhibitor, with an IC50 value of 0.05 nM. Porcn-IN-2 can be used for research of cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia, etc[1].
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.
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 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K[1].
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects[1][2][3].
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
Salinomycin is an anticoccidial drug with potent anti-bacterial activity and an novel anticancer agent targeting human cancer stem cells.
Hematein is a oxidation product of hematoxylin acted as a dye[1]. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells[2].
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities[1].
β-catenin inhibitor C2 is a novel potent selective β-catenin inhibitor with Kd of 54.96 nM, directly to ARM domain of β-catenin.β-catenin inhibitor C2 reduced viability of DLD1 and SW480 cells in dose-dependent manner with IC50 ranging between 0.8-1.3 uM, viability of HCT116 and SW48 with IC50 3.45-5.35 uM.β-catenin inhibitor C2 selectively inhibits β-catenin, lowers its cellular load and significantly reduces viability of β-catenin-driven cancer cells.
Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP[1].
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities[1].
Adavivint is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1]
Fz7-21S is a negative control of Fz7-21. Fz7-21 is a potent peptide antagonist of FZD7 receptors[1].
Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells[1][2].
Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC50 of 74 pM.
CHIR-99021 is a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM，showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases.
Box5 is a Wnt5a-derived N-butyloxycarbonyl hexapeptide (t-Boc-Met-Asp-Gly-Cys-Glu-Leu), acts as an Wnt5a antagonist; abolishes exogenous Wnt5a stimulation of A2058 cells increased adhesion, migration and invasion, all crucial components of tumor metastasis, also inhibits the basal migration and invasion of Wnt5a-expressing HTB63 melanoma cells, antagonizes the effects of Wnt5a on melanoma cell migration and invasion by directly inhibiting Wnt5a-induced PKC and Ca(2+) signaling.
CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat[1].
Cardionogen 1 (CDNG1/vuc230) is a Wnt signaling pathway inhibitor that slows down Myc-induced liver tumorigenesis. Cardionogen 1 treatment of zebrafish embryos before gastrulation inhibits cardiomyocyte formation, whereas treatment during or after gastrulation induces cardiomyocyte formation. Cardionogen 1 has potential in research into cancer and cardiovascular disease[1][2].
NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.IQ 1 maintains the pluripotency of murine ESCs in long-term culture in a Wnt-dependent manner. IQ 1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89.IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. IQ 1 thereby diminishes the β-catenin/p300 interaction and prevents β-catenin coactivator switching from CBP to p300.
NSC668036 is a Dishevelled (Dvl) PDZ domain inhibitor with a Kd of 237 µM. NSC668036 blocks Wnt signaling by interrupting the Frizzled-Dvl interaction[1].
UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; displays 63-fold and 175-fold selectivity over β-catenin/E-cadherin and β-catenin/APC interactions, respectively.
ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.