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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
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.

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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