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 |
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H9431 |
NRX-103094 |
NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM. |
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H8178 |
β-catenin-IN-37 |
1783856-40-5 | β-catenin-IN-37 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 17 uM; suppresses canonical Wnt signaling, downregulates the expression of Wnt target genes; inhibits the growth of Wnt-activated cancer cells with the IC50 values of 26 uM and 31 uM for SW480 and HCT116 cells, respectively. |
H8177 |
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. |
H8176 |
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). |
H8175 |
ZINC02092166 |
354543-09-2 | ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type β-catenin), respectively; remain affinity for muant catenin V511S, V511S/I569S and R469A with Ki of 20-50 uM; exhibits dual selectivity for β-catenin/Tcf over β-catenin/cadherin and β-catenin/APC PPIs. |
H8174 |
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. |
H8173 |
UU-T03 |
1586007-00-2 | UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin D1, and c-Myc in dose-dependent manners in SW480 cells. |
H8172 |
UU-T02 |
1500080-17-0 | UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; displays 63-fold and 175-fold selectivity over β-catenin/E-cadherin and β-catenin/APC interactions, respectively. |
H8171 |
UU-T01 |
1417162-83-4 | UU-T01 is a novel small-molecule inhibitor of β-catenin/Tcf4 protein-protein interaction with Ki of 3.14 uM, binds to β-catenin with Kd of 0.531 uM. |
H8170 |
Triptonide |
38647-11-9 | A key bioactive small molecule identified in Tripterygium wilfordii Hook F., has a broad spectrum of biological functions; effectively inhibits canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin; upregulates the expression of IL-37; potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively. |
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