β-catenin

CHIR-99021 (CT99021) is an activator of the Wnt β-catenin signaling pathway and a GSK-3α β inhibitor (IC50=10 6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33 Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

NRX-252114 (NRX252114) induces degradation of mutant β-catenin NRX-252114 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, and is able to enhance the binding of pSer33 S37A β-catenin to β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. Kd is 0.4 nM.

NRX-103095 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and enhances the affinity of pSer33 Ser37 β-catenin for β-TrCP with an EC50 of 163 nM.

Miclxin (DS37262926) is a novel MIC60 inhibitor that induces apoptosis through mitochondrial stress in mutant tumor cells via β-catenin.Miclxin is a potent inhibitor of mutant β-catenin, which is involved in the Wnt signaling pathway.Miclxin induces β-catenin-dependent apoptosis, leading to mitochondrial damage and loss of mitochondrial membrane. Miclxin has anti-tumor activity and kills tumors by targeting MIC60.

(E)-Ferulic acid ((E)-Coniferic acid) causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin.t(E)-Ferulic acid exert both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.

Wnt β-catenin agonist 1 is an agonist of Wnt β-catenin signalling pathway(EC50 of 0.27 μM).

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11 4 nM). XAV-939 selectively inhibits Wnt β-catenin-mediated transcription.

Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt beta-catenin pathway with potential antineoplastic activity.

β-catenin modulator IIa-661 is a small molecule inhibitor of the Wnt pathway with antitumour activity.

β-catenin CBP-IN-1 is a potent and selective inhibitor of CBP β-catenin

Toxoflavin (Xanthothricin) is an antagonist of the transcription factor 4 (TCF4) β-catenin complex and also inhibits KDM4A.

Wnt β-catenin-IN-5 (Compound 4) functions as an inhibitor of the Wnt β-catenin signaling pathway. This compound effectively eradicates colorectal cancer stem cells and inhibits tumor growth by suppressing the Wnt signaling pathway. Additionally, Wnt β-catenin-IN-5 promotes the degradation of KDM3A and KDM3B.

β-catenin-IN-8 (Compound 25) is an inhibitor of β-catenin. It effectively lowers the levels of both β-catenin and c-Myc proteins and suppresses Wnt target genes (Fgf20 and Sall4). Additionally, β-catenin-IN-8 exhibits anticancer activity against colorectal cancer and possesses metabolic stability.

β-Cateninmodulator-8 (Compound Ⅸa) is a β-Catenin modulator useful in cancer research.

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.

Wnt β-catenin activator 1 (Compound 5m) is an orally active activator of the Wnt β-catenin signaling pathway. It induces cell cycle arrest in the G1 phase, inhibits early proliferation of adipocytes, and suppresses adipogenesis in 3T3-L1 cells with an IC50 of 330 nM. In a high-fat diet-fed Syrian golden hamster model, Wnt β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities.

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.

Wnt β-catenin agonist 2 activates Wnt β-catenin signaling and is an effective Wnt agonist. Wnt β-catenin agonist 2 can be used in the study of diseases related to signal transduction and is closely related to cancer invasion and metastasis.

1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1 2 and p38 MAPK inhibitors.

Wnt β-catenin agonist 4 is an agonist of Wnt that activates Wnt β-catenin signaling and directs signaling.

β-catenin-IN-3 is a selective and potent β-catenin inhibitor (KD: 54.96 nM) that targets a cryptic regulatory site of β-catenin and significantly reduces the viability of β-catenin-driven cancer cells.

β-Catenin-IN-4 is a β-catenin inhibitor characterized by a K_i value of 0.64 μM. This compound effectively lowers the protein expression levels of cyclin D1 and c-Myc.

β-Catenin-IN-6 is an inhibitor of the canonical Wnt β-catenin signaling pathway, effectively impeding the proliferation of human colorectal cancer cells and demonstrating efficacy in a β-catenin RK3E mouse model [1] [2].