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.

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.

SKL2001, an agonist of the Wnt/β-catenin pathway, can disrupt the Axin/β-catenin interaction.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

DK419 is an orally active inhibitor of Wnt/β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK.

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

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.

NRX-252262 is a potent enhancer of the interaction between β-Catenin and its cognate E3 ligase, SCFβ-TrCP, inducing mutant β-Catenin degradation (EC50: 3.8 nM).

Nefopam hydrochloride (Nefopam HCl) is the hydrochloride salt form of nefopam, a centrally-acting, non-opioid benzoxazocine with analgesic activity.

(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).

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

FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects.

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

C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.

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

KY1220 destabilizes both β-catenin and Ras by targeting the Wnt/β-catenin pathway. It has an IC50 of 2.1 μM in HEK293 reporter cells.

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

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

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-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.