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
S6898 RCM-1 <1 mg/mL 60 mg/mL '''<1 mg/mL
S8968 PRI-724 <1 mg/mL 100 mg/mL 2 mg/mL
S7981 CCT251545 <1 mg/mL 30 mg/mL '''5 mg/mL
S6745 JW55 <1 mg/mL 87 mg/mL 4 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
S3842 Isoquercitrin -1 mg/mL 92 mg/mL -1 mg/mL
S8429 PNU-74654 <1 mg/mL 64 mg/mL 10 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
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
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
S3223 L-Quebrachitol -1 mg/mL 100 mg/mL '''-1 mg/mL
S3238 Resibufogenin -1 mg/mL 100 mg/mL '''-1 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
S7421 CGP 57380 <1 mg/mL 48 mg/mL '<1 mg/mL
S7954 CP21R7 (CP21) <1 mg/mL 63 mg/mL '''1 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

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 (NVP-XAV939) 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.

S6898

RCM-1

RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. RCM-1 decreases carcinogenesis and nuclear β-catenin.

S8968

PRI-724

PRI-724 is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

S7981

CCT251545

CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

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).

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.

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.

S8129

Salinomycin (from Streptomyces albus)

Salinomycin (Coxistac, Bio-cox), 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)

Adavivint (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.

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.

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.

S3223

L-Quebrachitol

L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.

S3238

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

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.

S7421

CGP 57380

CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.

S7954

CP21R7 (CP21)

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

S8178

Wnt agonist 1

Wnt agonist 1 (BML-284 HCL, AMBMP HCL) 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.

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 (NVP-XAV939) 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.

S6898

RCM-1

RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. RCM-1 decreases carcinogenesis and nuclear β-catenin.

S8968

PRI-724

PRI-724 is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

S7981

CCT251545

CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

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).

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.

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.

S8129

Salinomycin (from Streptomyces albus)

Salinomycin (Coxistac, Bio-cox), 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)

Adavivint (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.

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.

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,

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

2020, S1934-5909(20)30447-1

S3223

L-Quebrachitol

L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.

S3238

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

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,

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

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

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.

S7421

CGP 57380

CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.

2020, 11(4):990-996

2018, 26(16):4602-4614

2016, 10.1016/j.canlet.2016.02.052

S7954

CP21R7 (CP21)

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

2020, 15;8:309

2020, 4;526(3):764-771

2020, 29

S8178

Wnt agonist 1

Wnt agonist 1 (BML-284 HCL, AMBMP HCL) 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, 2020:8409239

2020, 10.1080/19490976

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, 8:647

2020, 10.1002

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.

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