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Wnt/beta-catenin

The Wnt signaling pathways are a group of signal transduction pathways which begin with proteins that pass signals into a cell through cell surface receptors. The name Wnt is a portmanteau created from the name Wingless and the name Int-1. Wnt signaling pathways use either nearby cell-cell communication (paracrine) or same-cell communication (autocrine). They are highly evolutionarily conserved in animals, which means they are similar across animal species from fruit flies to humans.

CHIR-99021
T2310252917-06-9
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.
  • $36
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ICG-001
T6113780757-88-2
ICG001 is a β-catenin TCF-mediated transcription inhibitor that selectively blocks β-catenin CBP interaction without interfering with β-catenin p300 interaction. It specifically binds to CREB protein with an IC50 of 3 μM.
  • $30
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XAV-939
T1878284028-89-3
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.
  • $48
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Heparan Sulfate
T193559050-30-0
Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG) that is tightly attached to cell surface or extracellular matrix proteins.
  • $44
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Ginkgetin
T4S2126481-46-9
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
  • $120
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IWR-1
T26511127442-82-3
IWR-1 (IWR-1-endo), a Wnt pathway inhibitor, stabilizes the Axin destruction complex(EC50=0.2 uM).
  • $50
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SRI 37892
T96621030769-75-5In house
SRI 37892 is a Fzd7 inhibitor with potent activities against Wnt/β-catenin signaling and cancer cell viability.
  • $397
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Triptonide
T5S105838647-11-9
1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1 2 and p38 MAPK inhibitors.
  • $51
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Toxoflavin
T1714284-82-2
Toxoflavin (Xanthothricin) is an antagonist of the transcription factor 4 (TCF4) β-catenin complex and also inhibits KDM4A.
  • $91
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TNIK-IN-5
T98102754265-66-0In house
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.
  • $129
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Tegatrabetan
T56421227637-23-1
Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.
  • $34
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Laduviglusib trihydrochloride
T226571782235-14-6
Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt β-catenin signaling. Laduviglusib trihydrochloride induces autophagy.
  • $36
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ZW4864 free base
T96422632259-92-6In house
ZW4864 (free base) is an orally active and selective β-catenin B-Cell lymphoma 9 protein-protein interaction (β-catenin BCL9 PPI) inhibitor, with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM [1]. ZW4864 (free base) also demonstrates good pharmacokinetic properties.
  • $163
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Xanthatin
T3S015326791-73-1
1. Xanthatin has cytotoxic activity. 2. Xanthatin has antibacterial and antifungal activies against MRSA. 3. Xanthatin may have therapeutic potential against NSCLC. 4. Xanthatin can inhibit murine melanoma B16-F1 cell proliferation possibly associated wit
  • $44
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NRX-252114
T635162763260-39-3In house
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.
  • $196
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CCT251545
T149071661839-45-7
CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).
  • $35
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MSAB
T8710173436-66-3
MSAB is a selective inhibitor of Wnt β-catenin signaling. MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt β-catenin target genes.
  • $31
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Echinacoside
T171682854-37-3
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.
  • $70
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ABC99
T236022331255-53-7
ABC99 is a selective irreversible inhibitor of the wnt-deacylating enzyme. ABC99 inhibited NOTUM (IC50: 13 nM). It also showed excellent selectivity across the serine hydrolase family.
  • $175
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C-82
T106411422253-37-9
C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
  • $453
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IWP-2
T2702686770-61-6
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.
  • $43
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EMT inhibitor-1
T111901638526-21-2
EMT inhibitor-1 is a compound that inhibits Hippo and Wnt signaling pathways, as well as TGF- macrophages (TGF-), exhibiting antitumor activity.
  • $113
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Adavivint
T56361467093-03-3
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.
  • $40
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IWP-4
T4245686772-17-8
IWP-4 (Inhibitor of Wnt Production-4) is a potent Wnt inhibitor.
  • $42
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Wnt-C59
T22421243243-89-1
Wnt-C59 (C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.
  • $33
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DK419
T151372102672-22-8In house
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.
  • $79
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Nesuparib
T619322055357-64-5
Nesuparib (JPI-547/OCN-201) is a potent PARP inhibitor with inhibitory effects on PARP and TNKS1.Nesuparib has antitumor activity and can be used in the treatment of tumors, endocrine and metabolic disorders, genitourinary disorders, and can be used in the study of neuropathic pain, neurodegenerative disorders, and cardiovascular diseases.
  • $90
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JW 67
T22884442644-28-2
JW 67 is an inhibitor of canonical Wnt pathway signaling. JW 67 rapidly reduced active β-catenin with a subsequent downregulation of Wnt target genes, including AXIN2, SP5, and NKD1.
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Wogonin
T2933632-85-9
Wogonin (Vogonin) is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties.
  • $50
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Pyrvinium pamoate
T73333546-41-6
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.
  • $31
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KY19382
T90252226664-93-1
KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
  • $100
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Fz7-21
TP12632247635-23-8
Fz7-21 ((Ac)-LPSDDLEFWCHVMY-NH2) is a peptide antagonist of FZD7 . It antagonises WNT3A-induced Wnt-β-catenin signalling in HEK293 expressing FZD7. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • $68
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DIF-3
T60485113411-17-9
DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
  • $93
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NCB-0846
T40111792999-26-8
NCB-0846 is an orally active TNIK inhibitor (IC50: 21 nM).
  • $31
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NRX-103095
T637302763260-38-2In house
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.
  • $153
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ISX-9
T2003832115-62-5
ISX-9 (Isoxazole 9) is essential for activating neuron-specific genes and serves as a neurogenesis inducer.
  • $41
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Nefopam hydrochloride
T047023327-57-3
Nefopam hydrochloride (Nefopam HCl) is the hydrochloride salt form of nefopam, a centrally-acting, non-opioid benzoxazocine with analgesic activity.
  • $37
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BML-284 hydrochloride
T88202095432-75-8
BML-284 hydrochloride (Wnt agonist 1 HCL) is a potent, selective Wnt canonical signaling activator and tubulin polymerization inhibitor.
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SKL2001
T6989909089-13-0
SKL2001, an agonist of the Wnt β-catenin pathway, can disrupt the Axin β-catenin interaction.
  • $34
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β-catenin-IN-2
T96961458664-10-2
β-catenin-IN-2, a potent inhibitor of β-catenin, is suitable for use in colorectal cancer research.
  • $97
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BML-284
T3144853220-52-7
BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.
  • $55
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WAY-262611
T19711123231-07-1
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.
  • $58
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SSTC3
T130041242422-09-8
SSTC3 is a casein kinase 1α (CK1α) activator and a potent HIF1α inhibitor, each with a Kd of 32 nM. It has potential antitumor activity, inhibits WNT signaling, and suppresses SHH medulloblastoma tumor growth.
  • $149
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TNIK-IN-3
T95562754265-25-1In house
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].
  • $108
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iCRT 14
T4486677331-12-3
iCRT 14 is a novel and potent inhibitor of β-catenin-responsive transcription (CRT) with an IC50 of 40.3 nM in assays of Wnt pathway activity.
  • $30
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NVP-TNKS656
T32611419949-20-4
NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor.
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Gossypolone
T319874547-72-2In house
Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch Wnt signaling and induces apoptosis.
  • $195
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FzM1
T240761680196-54-6In house
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.
  • $35
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