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.

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.

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.

(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.

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.

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

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-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.

β-Cateninmodulator-7 (Compound 5) acts as a regulator of β-catenin. It suppresses the expression of β-catenin in both the cytoplasm and nucleus of HCT-116 cells and inhibits the phosphorylation of GSK 3β. Additionally, β-Cateninmodulator-7 facilitates the release of NO in HCT-116 cells and inhibits the proliferation of these cancer cells, with an IC50 value of 0.6-0.9 μM. This compound is utilized in research related to colon cancer.

PTK7/β-catenin-IN-1 (compound 01065) is a potent inhibitor targeting PTK7/β-catenin and p53/MDM2, with IC50 values of 8.9 μM and 56.5 μM, respectively. This compound shows promise for cancer research applications [1].

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-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].

β-Catenin Modulator-5 (Compound IIa-84), an oxazole and thiazole-based compound, serves as a potent and selective modulator of β-Catenin [1].

β-Catenin modulator-1 (IIa-650) is a valuable agent in cancer research for modulating β-Catenin [1].

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.

PTK7 β-catenin-IN-6 (Compound 03653) acts as an inhibitor of the PTK7 β-catenin interaction, thereby disrupting the Wnt signaling pathway. It has demonstrated anticancer effects specifically targeting colorectal cancer (CRC) [1].

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].

Wnt β-catenin-IN-2 (Compound 3235-0367) serves as an inhibitor of the Wnt β-catenin signaling pathway, exhibiting IC50 and KD values of 7.1 and 2.5 μM, respectively. It is applicable in cancer research [1].

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-Catenin modulator-3 (compound IIa-112), an oxazole and thiazole-based chemical entity, serves as a potent and selective modulator of β-Catenin [1].

hCA Wnt β-catenin-IN-1 (Compd 15) is an inhibitor selectively targeting hCA isoforms II, IX, and XII, with K i values of 33.6, 24.1, and 6.8 nM, respectively. It also attenuates P-gp activity, disrupts the Wnt β-catenin signaling pathway, and compromises the viability of cancer cells, specifically against the NCI ADR-RES DOX-resistant cell line [1].