Wnt/beta-catenin

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Wnt/beta-catenin Products

New Wnt/beta-catenin Products
Catalog No. Information Product Use Citations Product Validations
S1180

XAV-939

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

S2662

ICG-001

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

S7086

IWR-1-endo

IWR-1-endo is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.

S7037

Wnt-C59 (C59)

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.

S7143

LGK-974

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.

S8704New

iCRT14

iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.

S8761New

Adavivint (SM04690)

SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.

S9416New

Triptonide

Triptonide, isolated from the roots of Tripterygium wilfordii, can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It is also an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent.

S7096

KY02111

KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.

S7085

IWP-2

IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses.

S7301

IWP-L6

IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM.

S3842

Isoquercitrin

Isoquercitrin, a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation.

S8429

PNU-74654

PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.

S7954

CP21R7 (CP21)

CP21R7, also known CP21, is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.

S8129

Salinomycin (from Streptomyces albus)

Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.

S7484

FH535

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

S8645

IWP-O1

IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells.

S8474

LF3

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.

S7490

WIKI4

WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.

S8262

PRI-724

PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.

S8644

GNF-6231

GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.

S8248

IQ-1

IQ-1 enables Wnt/β-catenin-driven expansion of mouse ESCs and prevents spontaneous differentiation, Maintains embryonic stem cell (ESC) pluripotency in Wnt3a-treated cells and prevents PP2A/Nkd interaction.

S8327

KYA1797K

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

S3630

Methyl Vanillate

Methyl Vanillate, one of the ingredients in Hovenia dulcis Thunb, activates the Wnt/β-catenin pathway and induces osteoblast differentiation in vitro.

S8178

Wnt agonist 1

Wnt agonist 1 is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.

S8647

iCRT3

iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.

S5815New

WAY-316606

WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb.

S8320

SKL2001

SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.

Catalog No. Information Product Use Citations Product Validations
S1180

XAV-939

XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

S2662

ICG-001

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

S7086

IWR-1-endo

IWR-1-endo is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.

S7037

Wnt-C59 (C59)

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.

S7143

LGK-974

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.

S8704New

iCRT14

iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.

S8761New

Adavivint (SM04690)

SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.

S9416New

Triptonide

Triptonide, isolated from the roots of Tripterygium wilfordii, can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It is also an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent.

S7096

KY02111

KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.

S7085

IWP-2

IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses.

S7301

IWP-L6

IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM.

S3842

Isoquercitrin

Isoquercitrin, a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation.

S8429

PNU-74654

PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.

S7954

CP21R7 (CP21)

CP21R7, also known CP21, is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.

S8129

Salinomycin (from Streptomyces albus)

Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.

S7484

FH535

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

S8645

IWP-O1

IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells.

S8474

LF3

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.

S7490

WIKI4

WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.

S8262

PRI-724

PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.

S8644

GNF-6231

GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.

S8248

IQ-1

IQ-1 enables Wnt/β-catenin-driven expansion of mouse ESCs and prevents spontaneous differentiation, Maintains embryonic stem cell (ESC) pluripotency in Wnt3a-treated cells and prevents PP2A/Nkd interaction.

S8327

KYA1797K

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

Catalog No. Information Product Use Citations Product Validations
S3630

Methyl Vanillate

Methyl Vanillate, one of the ingredients in Hovenia dulcis Thunb, activates the Wnt/β-catenin pathway and induces osteoblast differentiation in vitro.

S8178

Wnt agonist 1

Wnt agonist 1 is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.

Catalog No. Information Product Use Citations Product Validations
S8647

iCRT3

iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.

Catalog No. Information Product Use Citations Product Validations
S5815New

WAY-316606

WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb.

S8320

SKL2001

SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.

Tags: Wnt inhibition | Wnt signaling | Wnt pathway | Wnt cancer | beta-catenin signaling | beta-catenin pathway | beta-catenin cancer | Wnt beta-catenin pathway | Wnt activation | Wnt tumor | beta-catenin activation | beta-catenin tumor | beta-catenin phosphorylation | Wnt activity | β-catenin signaling | beta-catenin mutation | Wnt assay | Wnt mutation | Wnt drug | beta-catenin assay | Wnt inhibitors clinical trials | Wnt inhibitor review