Wnt/beta-catenin

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1180 XAV-939 <1 mg/mL 12 mg/mL '<1 mg/mL
S2662 ICG-001 <1 mg/mL 100 mg/mL '10 mg/mL
S2788 Capmatinib (INCB28060) <1 mg/mL 2 mg/mL '<1 mg/mL
S7086 IWR-1-endo <1 mg/mL 21 mg/mL <1 mg/mL
S6745 JW55 <1 mg/mL 87 mg/mL 4 mg/mL
S6616 ETC-159 <1 mg/mL 78 mg/mL '<1 mg/mL
S7037 Wnt-C59 (C59) <1 mg/mL 76 mg/mL <1 mg/mL
S7143 LGK-974 <1 mg/mL 79 mg/mL <1 mg/mL
S7096 KY02111 <1 mg/mL 75 mg/mL <1 mg/mL
S7085 IWP-2 <1 mg/mL 4 mg/mL '<1 mg/mL
S7301 IWP-L6 <1 mg/mL 25 mg/mL <1 mg/mL
S3842 Isoquercitrin -1 mg/mL 92 mg/mL -1 mg/mL
S8429 PNU-74654 <1 mg/mL 64 mg/mL 10 mg/mL
S7954 CP21R7 (CP21) <1 mg/mL 63 mg/mL 1 mg/mL
S8129 Salinomycin (from Streptomyces albus) <1 mg/mL 100 mg/mL 79 mg/mL
S8761 Adavivint (SM04690) <1 mg/mL 30 mg/mL <1 mg/mL
S7484 FH535 <1 mg/mL 72 mg/mL <1 mg/mL
S8645 IWP-O1 <1 mg/mL 86 mg/mL 86 mg/mL
S8474 LF3 <1 mg/mL 83 mg/mL 5 mg/mL
S7490 WIKI4 <1 mg/mL 7 mg/mL <1 mg/mL
S9416 Triptonide -1 mg/mL 71 mg/mL -1 mg/mL
S8644 GNF-6231 <1 mg/mL 89 mg/mL 5 mg/mL
S8248 IQ-1 <1 mg/mL 72 mg/mL '7 mg/mL
S8327 KYA1797K <1 mg/mL 7.2 mg/mL <1 mg/mL
S8704 iCRT14 <1 mg/mL 37 mg/mL <1 mg/mL
S2924 CHIR-99021 (CT99021) HCl <1 mg/mL 93 mg/mL '2 mg/mL
S1263 CHIR-99021 (CT99021) <1 mg/mL 10 mg/mL <1 mg/mL
S3630 Methyl Vanillate 12 mg/mL 36 mg/mL 36 mg/mL
S7914 Isoxazole 9 (ISX-9) <1 mg/mL 46 mg/mL '13 mg/mL
S8178 Wnt agonist 1 <1 mg/mL 77 mg/mL <1 mg/mL
S8647 iCRT3 <1 mg/mL 78 mg/mL 78 mg/mL
S5815 WAY-316606 <1 mg/mL 90 mg/mL 7 mg/mL
S8320 SKL2001 <1 mg/mL 57 mg/mL 57 mg/mL
S0458 KY1220 <1 mg/mL 63 mg/mL ''''<1 mg/mL
S2431 TMTD (Tetramethylthiuram disulfide) <1 mg/mL 48 mg/mL ''<1 mg/mL

Wnt/beta-catenin製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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. ICG-001 induces apoptosis.

S2788

Capmatinib (INCB28060)

Capmatinib (INCB28060) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.

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.

S6745

JW55

JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).

S6616

ETC-159

ETC-159 is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells.

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.

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. IWP-2 specifically inhibits CK1δ.

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.

S8761

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.

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.

S9416

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.

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).

S8704

iCRT14

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

S2924

CHIR-99021 (CT99021) HCl

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

S1263

CHIR-99021 (CT99021)

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

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.

S7914

Isoxazole 9 (ISX-9)

Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.

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.

S5815

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.

S0458

KY1220

KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.

S2431

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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. ICG-001 induces apoptosis.

S2788

Capmatinib (INCB28060)

Capmatinib (INCB28060) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.

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.

S6745

JW55

JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).

S6616

ETC-159

ETC-159 is an orally available, potent porcupine inhibitor with an IC50 of 2.9 nM for inhibiting β-catenin reporter activity in STF3A cells.

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.

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. IWP-2 specifically inhibits CK1δ.

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.

S8761

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.

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.

S9416

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.

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).

S8704

iCRT14

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

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2924

CHIR-99021 (CT99021) HCl

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

2020, 30;181(3):621-636

2020, 27(1):50-63.e5

2020, 30(1):21-33

S1263

CHIR-99021 (CT99021)

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

2020, 30;181(3):621-636.e22.

2020, 30;181(3):621-636

2020, 52(3):264-272

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.

S7914

Isoxazole 9 (ISX-9)

Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.

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.

2020, 10.1002/jcp.29550

2020, 10.1080/19490976

2019, 45:181-191

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

2017, 12(7):e0180897

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S5815

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.

2020, 24(10):5249-5258

2020, 10.1002

2019, 23(10):7088-7098

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S0458

KY1220

KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2431

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

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