Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
ABC99 is an N-hydroxyhydantoin (NHH) carbamate that selectively inhibits the Wnt-deacylating enzyme NOTUM (IC50=13 nM). ABC99 preserves Wnt3A signaling in the presence of NOTUM[1].
A negative allosteric modulator of the Frizzled4 (Fzd4) receptor and a Wnt/β-catenin pathway inhibitor with pEC50 value of 5.74 for inhibition of Wnt antagonism; induces conformational changes in Fz4 by interacting with the third intracellular loop, ICL3, inhibiting binding of dishevelled (Dsh) and hampering the formation of the Fz4-Dsh complex that is necessary for β-catenin nuclear transport and ultimately transcription of TCF/LEF-regulated genes.
KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.
Tabituximab barzuxetan (OTSA101-DTPA-90Y) is a radioimmunoconjugate composed of a humanized monoclonal antibody targeting FZD-10 (OTSA-101), and labeled with Yttrium 90. Tabituximab barzuxetan shows antineoplastic activity. Tabituximab barzuxetan can be used for synovial sarcoma research[1].
Desmethylicaritin is a phytoestrogenic molecule, has inducible effect on directional differentiation of embryonic stem cells into cardiomyocytes. Desmethylicaritin also suppresses adipogenesis via Wnt/β-catenin signaling pathway[1][2].
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells, suppressing the phosphorylation of Dvl2/3 and LRP6 in HeLa cells. IWP-O1 functions by preventing the secretion of Wnt proteins[1].
EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM.
iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
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.
Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[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].
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].
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].
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]
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.
Wnt/β-catenin agonist 4 (Derivative 83) is an agonist of Wnt that activates Wnt/β-catenin signal transmission[1].
NC-043 (15-Oxospiramilactone) is a diterpenoid derivative inhibitor of Wnt/β-catenin signaling that interferes with the β-catenin/TCF4 association; decreases the mRNA and/or protein expression of Wnt target genes Axin2, Cyclin D1 and Survivin in SW480 cells, inhibits anchorage-independent growth and xenograft tumorigenesis in vitro and in vivo; inhibits canonical Wnt signaling downstream of β-catenin stability, causes G2/M arrest and inhibits colon cancer cell growth.
β-catenin/CBP-IN-1 (CBP/β-catenin inhibitor) is a potent and selective CBP/β-catenin inhibitor, extracted from the patent WO2014092154A1. β-catenin/CBP-IN-1 has the potential for the study of liver fibrosis induced by hepatitis virus[1].
RA-V is a cyclic hexapeptide. RA-V has activity against Wnt, Myc and Notch with IC50 values of 50, 75, and 93 ng/mL, respectively. RA-V can be used for the research of cancer-related signaling pathways.
TNIK-IN-5 is an efficient TNIK inhibitor with IC50 of 0.05 μM. TNIK-IN-5 efficiently inhibits Wnt signaling in intact cells. TNIK-IN-5 shows excellent in vitro anti-colorectal cancer activity[1].
WIKI4 is a potent inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM).
FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities[1][2].
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs)[1].
Foxy-5 is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 is a WNT5A agonist and effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model[1][2].
iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.