β-catenin

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

β-catenin peptide(βCATp) acetate is a naturally occurring self-peptide presented by Kb that very efficiently mediates positive selection of the OT-I thymocytes.

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

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

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-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-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].

β-Catenin Modulator-2 (Compound IIa-130), which is an oxazole-thiazole derivative, serves as a potent and selective modulator of β-Catenin [1].

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].

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

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].

β-Catenin modulator-4 (compound IIa-92), containing oxazole and thiazole moieties, functions as a potent and selective β-Catenin modulator [1].

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

Wnt/β-catenin agonist 3 is a Wnt/beta-catenin agonist.

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

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.

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.

β-catenin peptide,(βCATp) is a naturally occurring self-peptide presented by Kb that very efficiently mediates positive selection of the OT-I thymocytes.

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.

Specnuezhenide (Nuezhenide) significantly protects human neuroblastoma SH-SY5Y cells from 6-hydroxydopamine-induced neurotoxicity.Nuezhenide is the main inhibitory compound of fruits, it shows a clear inhibitory effect to the seeds of wheat and Chinese cabbage.

Pyrvinium pamoate (Pyrvinium embonate) is an old anthelminthic medicine for the treatment of enterobiasis , which re-attracts attention as an anti-cancer drug due to its inhibition of Wnt β-catenin pathway in some types of cancer.

Methyl vanillate is Hovenia Dulcis Thunb extract and its ingredient methyl vanillate activate Wnt/β-catenin pathway and increase bone mass in growing or ovariectomized mice. Methyl vanillate is considered to be a slightly soluble (in water) acidic compound. Methyl vanillate can be synthesized from vanillic acid. Methyl vanillate has been identified in foods such as cow's milk and beer.

(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.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

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

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

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

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Foxy-5 Ammonium Salt is a WNT5A agonist, a mimetic peptide of WNT5A, a non-classical member of the Wnt family.Foxy-5 Ammonium Salt triggers cytoplasmic free calcium signaling without affecting β-catenin activation and inhibits migration and invasion of epithelial cancer cells.Foxy-5 Foxy-5 Ammonium Salt effectively reduces the metastatic spread of prostate cancer cells with low WNT5A expression in an in situ mouse model.

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt β-catenin pathway.

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.

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.

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.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

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-2663 enhances the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and increases the binding affinity of β-catenin to β-TrCP (Kd: 54.8 nM, EC50: 22.9 nM).

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.

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).

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

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.

SRI 37892 is a Fzd7 inhibitor with potent activities against Wnt/β-catenin signaling and cancer cell viability.

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.

ZW4864 (free base) is an orally active and selective β-catenin B-Cell lymphoma 9 protein-protein interaction (β-catenin BCL9 PPI) inhibitor, with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM [1]. ZW4864 (free base) also demonstrates good pharmacokinetic properties.