wnt 6

KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂，Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。

MN-64 是一种有效的tankyrase 1抑制剂，对TNKS1、TNKS2、ARTD1 和 ARTD2 的IC50值分别为 6、72、19.1 和 39.4 μM。

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.

BMD4503-1 是喹喔啉的衍生物，可抑制LRP5 6-硬化蛋白(sclerostin)的相互作用，并调节Wnt信号通路。

PTK7 β-catenin-IN-6 (Compound 03653) 作为一类抑制PTK7 β-catenin相互作用的化合物，能有效地抑制Wnt信号通路，对结直肠癌 (CRC) 具有抗癌效果。

β-catenin-IN-6是一种针对Wnt β-catenin(典型的wingless相关整合位点)通路的抑制剂，能够抑制人类结直肠癌细胞的增殖，并在β-catenin RK3E小鼠模型上展现出效果。

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.

KP-6是一种多肽，同时也是Wnt β-catenin信号的抑制剂。KP-6能够抑制TGF-β，并阻断体内关键的快速纤维化信号通路。该化合物有效抑制肾组织损伤和肾纤维化，并逆转慢性肾病（CKD）的病程。

Carboxylesterase-IN-2 是一种有效的 Carboxylesterase Notum 抑制剂（IC50 ≤10 nM）。Carboxylesterase-IN-2具有研究癌症疾病的潜力。

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.

BMD4503-2 is an LRP5 6-sclerostin interaction inhibitor. BMD4503-2 recovers the downregulated activity of the Wnt β-catenin signaling pathway by competitively binding to the LRP5 6-sclerostin complex.