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|
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.
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.
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).
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.
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.
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.
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.
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.
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.
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.
No.1378 West Wenyi Road, Yuhang District, HangZhou, Zhejiang, China