wnt 6

Wnt/β-catenin-IN-6 (compound B10) is a potent inhibitor of the Wnt/β-catenin signaling pathway. It effectively suppresses the activity of A549 cells, with an IC50 of 1.28 μM.

MN-64 is a tankyrases inhibitor, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

BMD4503-1 is a quinoxaline derivative that can inhibit the interaction between LRP5 6 and sclerostin, thereby modulating the Wnt signaling pathway.

TNKS-IN-3 (Compound 6) is a TNKS2 inhibitor with a Ki of 8.5 nM. It demonstrates strong activity with an IC50 of 71 nM, effectively inhibiting the WNT/β-catenin signaling pathway, and is useful for research in cancer and fibrosis.

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt/β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg/kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

BMD4503-2 is a competitive inhibitor of the LRP5 6-sclerostin complex that restores the activity of the Wnt β-catenin signaling pathway and can be used for cancer research.

AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. Consistent with this lack of potencytowards tankyrase, AZ0108 is not active in a DLD-1 Wnt luciferase reporter assay.

Carboxylesterase-IN-2 is a potent Carboxylesterase Notum inhibitor (IC50 <= 10 nM).Carboxylesterase-IN-2 has potential for the study of cancer diseases.

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].

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].

9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α.

KP-6 is a peptide that acts as an inhibitor of the Wnt β-catenin signaling pathway. It suppresses TGF-β and disrupts key signals that lead to rapid fibrosis in vivo. KP-6 helps prevent kidney tissue damage and fibrosis, offering the potential to reverse the progression of chronic kidney disease (CKD).