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You are here:Home-Inhibitors & Agonists-Wnt/Notch/Hedgehog-Beta-catenin

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β-catenin is a dual function protein, regulating the coordination of cell–cell adhesion and gene transcription. In humans, the CTNNB1 protein is encoded by the CTNNB1 gene. β-catenin is a subunit of the cadherin protein complex and acts as an intracellular signal transducer in the Wnt signaling pathway. It is a member of the catenin protein family and homologous to γ-catenin. Mutations and overexpression of β-catenin are associated with many cancers, including hepatocellular carcinoma, colorectal carcinoma, lung cancer,malignant breast tumors, ovarian and endometrial cancer. β-catenin is regulated and destroyed by the beta-catenin destruction complex, and in particular by the adenomatous polyposis coli (APC) protein, encoded by the tumour-suppressing APC gene. Therefore genetic mutation of the APC gene is also strongly linked to cancers, and in particular colorectal cancer resulting from familial adenomatous polyposis (FAP).

Cat. No. Product Name CAS No. Information
GY03893

Toxoflavin

84-82-2

A novel small molecule inhibitor of Wnt/beta-catenin signaling that selectively disrupts β- catenin/Tcf4 interaction and inhibits its transcriptional activity; produces in vitro antitumor activity in a panel of cancer cells, reduces β-catenin nuclear localization and induces apoptosis, and inhibits expression of Tcf4 responsive genes.

GY03866

SKL2001

909089-13-0

SKL2001 is a specific small molecule activator (agonist) of the Wnt/β-catenin pathway, stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction; strongly activates β-catenin responsive transcription, upregulates TOPflash reporter activity without effect on the activity of FOPFlash with mutated β-catenin/Tcf-binding elements, as well as either NF-κB or p53 reporter activity; upregulates the expression of Axin2, inhibits N-terminal β-catenin phosphorylation without affecting GSK-3β activity; suppresses preadipocyte differentiation, the alternative mesenchymal differentiation pathway.

GY06669

ZTM000990

115834-23-6

ZTM000990 is a small-molecule antagonist of the oncogenic Tcf4/β-catenin protein complex with IC50 of 0.64 uM; reduces levels of either c-Myc or cyclin D1 in HCT116 cells without effect on cyclin E levels, shows effects on growth of colon and prostate cancer cell lines (IC50=0.15-0.3 uM).

GY06660

CCT-031374 hydrobromide

1219184-91-4

CCT-031374 hydrobromide is a novel small-molecule Wnt signaling inhibitor that inhibits TCF-dependent transcription with IC50 of 6.1 uM in 7dF3 reporter assay; promotes β-catenin degradation and lowers β-catenin levels in mouse L-cells, blockes the growth of a number of cancer cell lines including SW480 colon cancer cells (IC50=13.2 uM); blocks free β-catenin levels in BIO-stimulated HEK293 cells.

GY06657

Tegatrabetan

1227637-23-1

Tegatrabetan (BC-2059, BC2059, Tegavivint) is an orally bioavailable β-catenin antagonist that disrupts the binding of β-catenin to TBL1 and promotes β-catenin degradation, attenuates nuclear and cytoplasmic levels of β-catenin; reduces transcriptional activity of TCF4 and expression of its target genes, cyclin D1, c-MYC and survivin. BC treatment dose-dependently induced apoptosis of cultured and primary AML BPCs; significantly improves the median survival of immune-depleted mice engrafted with either cultured or primary AML BPCs.

GY06588

E-7386

1799824-08-0

E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively; exhibits anti-tumor activity in vitro tumor proliferation panel against 28 human tumor cell lines; modulates the expression of Wnt signaling pathway related genes including AXIN2 and other genes, significantly suppressed the number of polyposis in a dose dependent manner at the dose 8.5-50 mg/kg, also significantly changed the expressions of Wnt related genes in whisker follicle of ApcMin/+mice model.

GY06575

iCRT-5

18623-44-4

iCRT-5 is a selective, cell-permeable β-catenin responsive transcription (CRT) inhibitor with IC50 of 18 nM; specifically modulates the nuclear transcriptional activity of β-catenin while not affecting its cytoskeletal function in stabilizing adherens junctions at the cell membrane; blocks Wnt/β-catenin-induced target genes and phenotypes in various mammalian and cancer cell lines.

GY06569

β-catenin-IN-11a

1884472-26-7

β-catenin-IN-11a is a β-catenin/CD44/Nanog axis inhibitor, docks into the β-catenin allosteric site and interferes β-catenin/TCF-4 complex; blocks the cell cycle inhibitory effect of CD44 and induces cell accumulation of CD44 high cells in cycling phase in S, G2 and M phase, leads to inhibition of embryonic transcriptional factor Nanog but not Sox2 or Oct-4 in colon cancer cells.

GY02176

PNU-74654

113906-27-7

A novel potent Wnt/beta-catenin inhibitor by disrupting Tcf/β-catenin interaction; binds to β-catenin with Kd of 450 nM, significantly decreases NCI-H295 cell proliferation (96 h, IC50=69 nM), increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impaires CTNNB1/beta-catenin expression and increases beta-catenin target genes.

GY01846

WIKI4

838818-26-1

A novel small molecule inhibitor of the Wnt/β-catenin pathway by inhibiting the enzymatic activity of TNKS2; prevents auto-ADP-ribosylation of TNKS2 with IC50 of 15 nM; inhibits expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in cancer cell lines as well as in human embryonic stem cells.

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