tcf/β-catenin

TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

CCT 031374 hydrobromide is a TCF/β-catenin inhibitor with antitumor activities.

CWP232228, a potent and selective Wnt / β-catenin signaling inhibitor, antagonizes the binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 inhibits the formation and metastasis of tumors by inhibiting the growth of breast cancer and live

FzM1.8 is an allosteric FZD4 agonist with a pEC50 of 6.4. FzM1.8 binds to FZD4, promotes TCF/LEF transcriptional activity in the absence of any WNT ligand, and activates the WNT/β-catenin pathway.

WAY262611 is a Wnt/β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay.

CCT070535 inhibits TCF-dependent transcription at the TCF level, displaying GI50 values of 17.6 μM in HT29 (APC mutation), 11.1 μM in HCT116 (oncogenic β-catenin), 11.8 μM in SW480 (APC mutation), and 13.4 μM in SNU475 (Axin mutation) cells.

BML-286 is a WNT pathway modulator with potential anticancer activity, inducing β-catenin- and TCF-dependent transcriptional activity, and can be used in the study of degenerative diseases, intestinal, breast, bladder, gastric, melanoma, leukemia, hepatocellular carcinoma and nephroblastoma.

I-67, a structural isomer of I-66, is a potent β-catenin inhibitor with an IC50 of less than 50 nM. It disrupts the interaction between β-catenin and T cell factor (TCF) transcription factors and exhibits anticancer properties.

BRD1172 (ML320) is a selective inhibitor of GSK3β, exhibiting an IC50 of 24 nM, demonstrating greater potency against GSK3β compared to CDK5. It significantly inhibits GSK3β-mediated Tau phosphorylation in SH-SY5Y cells and reduces the negative regulation by GSK3β on β-catenin degradation and TCF/LEF promoter activity. BRD1172 is applicable in research on Alzheimer's disease, cardiac hypertrophy, and cancer.

RMC-9945 (RM-044) is a KRAS inhibitor that is selective, covalent, and orally active against the RAS(ON) G12D mutation. It enhances the transcriptional activity of β-Catenin/TCF and demonstrates sustained disease control in early liver metastasis models of colorectal cancer.

ICG001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

IWR-1 (IWR-1-endo) is a tankyrase inhibitor that targets the Wnt/β-catenin pathway, with an IC₅₀ of 180 nM. IWR-1 contributes to the activation of TCF/LEF and the expression of downstream targets of the Wnt/β-catenin pathway. IWR-1 promotes β-catenin phosphorylation by enhancing the stability of the Axin-mediated disassembly complex. IWR-1 can be used in research on diseases such as cancer and psoriasis.

β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively.

ICG001 is a β-catenin/TCF-mediated transcription inhibitor that selectively blocks β-catenin/CBP interaction without interfering with β-catenin/p300 interaction. It specifically binds to CREB protein with an IC50 of 3 μM.

CDK8-IN-11 is a selective and potent CDK8 inhibitor that shows antiproliferative activity in colon cancer cell lines, inhibiting WNT/β-catenin activation and TCF family transcriptional activity, inducing G1-phase arrest in HCT-116 cells, useful for colon cancer research.

UU-T01 is a selective inhibitor of the β-Catenin/T-cell factor 4 (β-catenin/Tcf) protein-protein interaction (PPI), exhibiting a Ki value of 3.14 µM, and directly binds to β-catenin with a KD value of 0.531 µM.

Streptonigrin is an aminoquinone antitumor and antibacterial antibiotic produced by Streptomyces flocculus. Streptonigrin inhibits β-Catenin/Tcf signaling and shows cytotoxicity in β-catenin-activated cells. Streptonigrin induces delayed chromosomal instability involving interstitial telomeric sequences in Chinese hamster ovary cells. Note: Streptonigrin from natural resource is (-)-rotation, has CAS#3930-19-6 and is a R-isomer.

Murayaquinone is a hepatitis C virus proteinase inhibitor and small molecule antagonist of the oncogenic Tcf/β-catenin protein complex.

β-Catenin-IN-7 (Compound 9) is an inhibitor of β-catenin that disrupts its interaction with Tcf-4, consequently impeding Wnt-dependent gene expression, and exhibits anticancer activity [1].

Pterostilbene-isothiocyanate is a pterostilbene derivative and Wnt/β-catenin pathway inhibitor. It disrupts β-catenin/TCF-4 interaction to inhibit tumor growth and migration.

BML-284 hydrochloride (Wnt agonist 1 HCL) is a potent, selective Wnt canonical signaling activator and tubulin polymerization inhibitor.

β-catenin-IN-2, a potent inhibitor of β-catenin, is suitable for use in colorectal cancer research.

fStAx-35R TFA is a hydrophobic carbon chain-stabilized peptide that inhibits the Wnt/β-catenin signaling pathway by disrupting the β-catenin-TCF interaction. This compound is utilized in cancer research.