Wnt/beta-catenin

信号通路图

研究领域

抑制剂选择性比较

Wnt/beta-catenin产品

所有产品 Wnt/beta-catenin抑制剂(26) Wnt/beta-catenin激活剂(5) Wnt/beta-catenin拮抗剂(1) Wnt/beta-catenin激动剂(2)

目录号	产品描述	文献引用	实验数据
S1180	XAV-939 XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，无细胞试验中IC50为11 nM/4 nM，调节轴蛋白水平，而对 CRE， NF-κB和TGF-β无作用。	Cancer Cell, 2020, 13;37(1):104-122e12 Nat Cell Biol, 2020, 11 Theranostics, 2020, 10(6):2553-2570	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
S2662	ICG-001 ICG-001 拮抗Wnt/β-catenin/TCF介导的转录，并特异性结合到启动子结合蛋白（CBP)，IC50为3 μM，但不能结合到相关的转录共激活因子p300上。ICG-001 可诱导凋亡。	Nat Commun, 2020, 27;11(1):1578 Theranostics, 2020, 10(2):484-497 Front Immunol, 2020, 27;11:438	ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.
S2788	Capmatinib (INCB28060) Capmatinib (INCB28060)是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。Capmatinib (INCB28060)可抑制 Wnt/β-catenin 和 EMT 信号通路并诱导c-MET扩增阳性的弥漫性胃癌中的凋亡。Phase 1。	Nat Commun, 2020, 25;11(1):1556 Genome Med, 2020, 18;12(1):17 Clin Cancer Res, 2020, 26(6):1408-1419	(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control).
S7086	IWR-1-endo IWR-1-endo是一种Wnt通路抑制剂，在表达 Wnt3A 的 L-细胞中IC50为180 nM，诱导Axin2蛋白水平，并通过稳定Axin骨架破坏复合体来促进β-catenin磷酸化。	Nat Cell Biol, 2020, 11 Nat Commun, 2020, 22;11(1):2585 Stem Cell Res Ther, 2020, 11(1):118	Effect of IWR-1 treatment on total β-catenin levels and adipogenesis in high-passage shSCR and shTCF7L2 cells. Cells were treated with IWR-1 (10 μmol/L) every other day for 6 days during differentiation. Western blot demonstrates the effect of IWR-1 on total β-catenin protein levels at the end of adipogenesis (each lane represents a single independent adipogenesis experiment, n = 4 for each treatment).
S8392^New	NCB-0846 NCB-0846是一种新型的、口服的Wnt小分子化合物抑制剂，抑制TNIK (TRAF2 and NCK-Interacting Kinase)的IC50为21 nM。
S6745^New	JW55 JW55是一种有效的、选择性经典Wnt信号通路抑制剂，通过抑制TNKS1/2的PARP区域发挥作用。
S6616^New	ETC-159 ETC-159是一种具有口服活性的porcupine抑制剂，在STF3A细胞中抑制β-catenin报告基因的活性，IC50为2.9 nM。
S8704^New	iCRT14 iCRT14是β-catenin/Tcf抑制剂，在HFP实验中Ki值为54 ± 5.2 μM。
S7037	Wnt-C59 (C59) Wnt-C59 (C59)是一种PORCN抑制剂，作用于Wnt3A介导的多聚TCF结合位点驱动的荧光素酶的激活，在 HEK293细胞中IC50为74 pM。	Biochim Biophys Acta Mol Cell Res, 2020, 26;1867(7):118711 Sci Total Environ, 2020, 6;725:138433 Environ Pollut, 2020, 261:114153	Application of XAV939 or Wnt-c59 with FGF2 blocks the accumulation of nuclear b-catenin in MGPCs, and increases levels of p38MAPK in Muller glia, whereas levels of cFos are unaffected. a, b, Eyes were injected with four consecutive daily injections of FGF2 6 XAV939 or Wnt-c59, BrdU 24 h after the last injection of FGF2, and retinas harvested 24 h later. Wnt-c59 (treated). a, b-catenin in the nuclei of Sox91 Muller glia/MGPCs on 70% grayscale background.
S7143	LGK-974 LGK-974是一种有效的特异性PORCN抑制剂,抑制Wnt信号通路，在TM3细胞中IC50为0.4 nM。Phase 1。	Genome Med, 2020, 18;12(1):17 Cell Rep, 2020, 12;31(6):107625 Cancers (Basel), 2020, 31;12(4)	Nestin silencing inhibits the Wnt/β-catenin signaling in breast CSC. Nestin-si and Nestin-c breast CSC were cultured for 48 h, and the relative levels of target proteins and phosphorylation were determined by western blotting. Data are presented as the mean ± SD of the levels of target proteins vs. the β-actin control, or the phosphorylated vs. the total form, from six separate experiments. In addition, Nestinhigh in the presence or absence of LGK974 (1 nM), Nestinlow in the presence or absence of SB216763 (5 uM), and control CSC were tested for their proliferation via mammosphere formation assays. Quantitative analysis of the formed mammospheres. *P <0.05, vs. the Nestin-c or control, except for specifically indicated. CSC, cancer stem cell; SD, standard deviation.
S7096	KY02111 KY02111抑制Wnt信号，促进hPSCs分化为心肌细胞，可能对APC和GSK3β的下游起作用。	Cell Physiol Biochem, 2018, 50(2):538-551 Exp Eye Res, 2015, 132C:174-178	Transient Wnt inhibition results in persistent decrease of b-catenin. HTM cells were incubated for 4 days in serum-free media, treated with Wnt inhibitors for 8 days in serum free media, and recovered for 4 days in serum-free media before being fixed and stained for b-catenin. (B) HTM cells treated with 10 μM KY02111 or LGK-974 likewise show a reduction of b-catenin staining intensity. (CeD) Quantification of b-catenin staining intensity in HTM cells from 3 donors indicates a statistically significant decrease in intensity after 0.5 μg/mL SFRP1 (SFRP1), 10 μM KY02111, and 10 μM LGK-974. (E) Western blot shows increased T41 phosphorylation of b-catenin after SFRP1 or KY02111 treatment. Data presented as mean ± SEM. Significant difference from control using Tukey's method denoted by * p < 0.05; ***p < 0.001; using Student's T-test denoted by #p < 0.05. n=3. Scale bar 50 μm.
S7085	IWP-2 IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响。IWP-2可特定低抑制 CK1δ。	Biomaterials, 2020, 249:120015 Cell Stem Cell, 2019, 24(3):447-461.e8. Nat Neurosci, 2019, 22(3):484-491	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
S7301	IWP-L6 IWP-L6是高效强效的Porcn的抑制剂，EC50为0.5 nM。
S3842	Isoquercitrin Isoquercitrin, a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation.
S8429	PNU-74654 PNU-75654通过抑制β-catenin和Tcf4的相互作用（Kd=450 nM）,破坏Wnt signaling pathway。	Cell Death Differ, 2020, 7 Br J Cancer, 2020, 122(4):578-589 Free Radic Res, 2019, 53(8):851-864
S7954	CP21R7 (CP21) CP21R7（CP21）是一种有效的、选择性的GSK-3β抑制剂，能有效激活经典Wnt信号通路。	Front Cell Dev Biol, 2020, 15;8:309 Biochem Biophys Res Commun, 2020, 4;526(3):764-771 Hum Cell, 2020, 29
S8129	Salinomycin (from Streptomyces albus) Salinomycin, 曾经被用作抗球虫药，具有抗癌和抗肿瘤干细胞的效果。	Biomed Pharmacother, 2020, 16;127:110225 Prostate, 2020, 80(3):267-273 EMBO Mol Med, 2019, 11(10):e9930	The salinomycin inhibited the growth of CNE-2 in time- and dose-dependent manner. SAL salinomycin
S8761	Adavivint (SM04690) SM04690是一种有效的经典Wnt信号通路抑制剂，抑制TCF/LEF报告基因的EC50为19.5 nM。在多种细胞实验中，它比其他已知的Wnt抑制剂更有效。
S7484	FH535 FH535是一种Wnt/β-catenin信号传导抑制剂，同时也是PPARγ和PPARδ的双重拮抗剂。	Gastroenterology, 2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc, 2019, 3(7):1246-1260 Gene, 2019, 684:95-103	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
S8645	IWP-O1 IWP-O1是porcn抑制剂，在培养细胞中进行的Wnt信号报告基因实验中，EC50为80 pM。它能有效地抑制Hela细胞中Dvl2/3的磷酸化。
S8474	LF3 LF3是一种特异的、对经典Wnt信号通路抑制剂，通过破坏β-catenin和Tcf4的相互作用发挥抑制作用，IC50<2 μM。	FASEB J, 2020, 2 Nat Cell Biol, 2019, 21(5):627-639 Carcinogenesis, 2019, 10.1093/carcin/bgz079
S7490	WIKI4 WIKI4 是新型的Tankyrase抑制剂，作用于TNKS2的IC50为15 nM ,且对Wnt/ß-catenin信号通路也有抑制作用。	Nat Commun, 2019, 10(1):4363
S9416	Triptonide Triptonide, isolated from the roots of Tripterygium wilfordii, can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It is also an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent.
S8644	GNF-6231 GNF-6231是一种有效的、具有口服活性的、选择性的Porcupine抑制剂，其IC50为0.8 nM。
S8248	IQ-1 IQ-1可以使小鼠胚胎干细胞在Wnt/β-catenin信号的驱使下扩增并阻止其非定向分化。在经Wnt3a处理的细胞中，维持维持胚胎干细胞(ESC)多能性、阻止PP2A/Nkd的相互作用。	Cell Mol Life Sci, 2019, 76(14):2817-2832
S8327	KYA1797K KYA1797K是一种有效的、高度选择性的Wnt/β-catenin抑制剂，在TOPflash实验中，IC50为0.75 μM。	Cell Div, 2020, 1;15:2 J Cell Biochem, 2020, 121(2):1250-1259 J Immunol, 2019, 203(10):2630-2643	A549 cells were treated with KYA1797K for 72 h, cells lysates were collected for western blotting, concentration gradient (1, 12.5 μM, 25 μM) was set for the analysis
S2924	CHIR-99021 (CT99021) HCl CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂，IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。	Cell, 2020, 30;181(3):621-636 Cell Res, 2020, 30(1):21-33 Nat Commun, 2020, 22;11(1):2585	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1263	CHIR-99021 (CT99021) CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。CHIR-99021 可作为Wnt/β-catenin的激活剂并诱导自噬。	Cell, 2020, 30;181(3):621-636.e22. Cell, 2020, 30;181(3):621-636 Nat Genet, 2020, 52(3):264-272	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S3630	Methyl Vanillate Methyl Vanillate是枳椇子成分之一，在体外能激活Wnt/β-catenin信号通路并诱导成骨分化。
S7914	Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9)是一种成体神经发生的合成促进剂，通过引起成熟神经干细胞/前体细胞(NSPCs)的神经元分化而发挥作用。Isoxazole 9 (Isx-9) 可激活多条信号通路，包括 TGF-β 诱导的上皮-间质转化信号通路 (EMT) ，以及在心脏分化不同阶段的经典和非经典的 Wnt 信号通路。
S8178	Wnt agonist 1 Wnt agonist 1是具有细胞透性的Wnt信号通路激活剂，诱导依赖于β-catenin-和TCF-的转录活性，EC50为0.7 μM。	J Cell Physiol, 2020, 10.1002/jcp.29550 Gut Microbes, 2020, 10.1080/19490976 EBioMedicine, 2019, 45:181-191	Both Wnt sinaling activators of agonist and recombinant protein, and therapeutic agents of fluorouracil and docetaxel stimulated TCF-4 promoter functions of wild-type (wt) could be blocked by Nano-Let-7b, compared with negative control group of mutant-type (mut). In detail, Let-7b alone affected the TCF-4 promoter activity effectively, and wnt signaling activators of either Wnt agonist-1 or Wnt protein attenuated the Let-7b functions significantly. Combined usage of therapeutic agent of either fluorouracil or docetaxel with Let-7b increased the TCF-4 activity when compared to groups treated with Let-7b alone, however, the TCF-4 activity when applying combination was still significantly lower than that of controlled group
S8647	iCRT3 iCRT3是Wnt/β-catenin信号的拮抗剂，在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。	PLoS One, 2017, 12(7):e0180897
S5815	WAY-316606 WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。
S8320	SKL2001 SKL2001是一种新型的Wnt/β-catenin信号通路的激动剂，破坏Axin/β-catenin的相互作用。	Eur Rev Med Pharmacol Sci, 2020, 24(10):5249-5258 J Cell Biochem, 2020, 10.1002 J Cell Mol Med, 2019, 23(10):7088-7098	Western blots of nuclear and cytoplasmic fractions of β-catenin and total CDH3. d The ratio of nuclear/cytosolic of β-catenin was calculated by densitometry analysis.
S2431^New	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) 可以通过降低肝脏指数来降低鸡的生长性能，而肾脏，心脏和脾脏指数均有增加。TMTD (Tetramethylthiuram disulfide) 通过改变 VEGF，HIF-1α 和 WNT4 的表达来诱发胫骨软骨发育不良 tibial dyschondrolplasia (TD)。TMTD (Tetramethylthiuram disulfide) 广泛应用于橡胶加工中作为低温硫化的超促进剂，且是农业生产中一种重要的农药。

目录号	产品描述	文献引用	实验数据
S1180	XAV-939 XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，无细胞试验中IC50为11 nM/4 nM，调节轴蛋白水平，而对 CRE， NF-κB和TGF-β无作用。	Cancer Cell,2020, 13;37(1):104-122e12 Nat Cell Biol,2020, 11 Theranostics,2020, 10(6):2553-2570	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
S2662	ICG-001 ICG-001 拮抗Wnt/β-catenin/TCF介导的转录，并特异性结合到启动子结合蛋白（CBP)，IC50为3 μM，但不能结合到相关的转录共激活因子p300上。ICG-001 可诱导凋亡。	Nat Commun,2020, 27;11(1):1578 Theranostics,2020, 10(2):484-497 Front Immunol,2020, 27;11:438	ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.
S2788	Capmatinib (INCB28060) Capmatinib (INCB28060)是一种新型的，ATP竞争性c-MET抑制剂，无细胞试验中IC50为0.13 nM，对RONβ，EGFR和HER-3无活性。Capmatinib (INCB28060)可抑制 Wnt/β-catenin 和 EMT 信号通路并诱导c-MET扩增阳性的弥漫性胃癌中的凋亡。Phase 1。	Nat Commun,2020, 25;11(1):1556 Genome Med,2020, 18;12(1):17 Clin Cancer Res,2020, 26(6):1408-1419	(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control).
S7086	IWR-1-endo IWR-1-endo是一种Wnt通路抑制剂，在表达 Wnt3A 的 L-细胞中IC50为180 nM，诱导Axin2蛋白水平，并通过稳定Axin骨架破坏复合体来促进β-catenin磷酸化。	Nat Cell Biol,2020, 11 Nat Commun,2020, 22;11(1):2585 Stem Cell Res Ther,2020, 11(1):118	Effect of IWR-1 treatment on total β-catenin levels and adipogenesis in high-passage shSCR and shTCF7L2 cells. Cells were treated with IWR-1 (10 μmol/L) every other day for 6 days during differentiation. Western blot demonstrates the effect of IWR-1 on total β-catenin protein levels at the end of adipogenesis (each lane represents a single independent adipogenesis experiment, n = 4 for each treatment).
S8392^New	NCB-0846 NCB-0846是一种新型的、口服的Wnt小分子化合物抑制剂，抑制TNIK (TRAF2 and NCK-Interacting Kinase)的IC50为21 nM。
S6745^New	JW55 JW55是一种有效的、选择性经典Wnt信号通路抑制剂，通过抑制TNKS1/2的PARP区域发挥作用。
S6616^New	ETC-159 ETC-159是一种具有口服活性的porcupine抑制剂，在STF3A细胞中抑制β-catenin报告基因的活性，IC50为2.9 nM。
S8704^New	iCRT14 iCRT14是β-catenin/Tcf抑制剂，在HFP实验中Ki值为54 ± 5.2 μM。
S7037	Wnt-C59 (C59) Wnt-C59 (C59)是一种PORCN抑制剂，作用于Wnt3A介导的多聚TCF结合位点驱动的荧光素酶的激活，在 HEK293细胞中IC50为74 pM。	Biochim Biophys Acta Mol Cell Res,2020, 26;1867(7):118711 Sci Total Environ,2020, 6;725:138433 Environ Pollut,2020, 261:114153	Application of XAV939 or Wnt-c59 with FGF2 blocks the accumulation of nuclear b-catenin in MGPCs, and increases levels of p38MAPK in Muller glia, whereas levels of cFos are unaffected. a, b, Eyes were injected with four consecutive daily injections of FGF2 6 XAV939 or Wnt-c59, BrdU 24 h after the last injection of FGF2, and retinas harvested 24 h later. Wnt-c59 (treated). a, b-catenin in the nuclei of Sox91 Muller glia/MGPCs on 70% grayscale background.
S7143	LGK-974 LGK-974是一种有效的特异性PORCN抑制剂,抑制Wnt信号通路，在TM3细胞中IC50为0.4 nM。Phase 1。	Genome Med,2020, 18;12(1):17 Cell Rep,2020, 12;31(6):107625 Cancers (Basel),2020, 31;12(4)	Nestin silencing inhibits the Wnt/β-catenin signaling in breast CSC. Nestin-si and Nestin-c breast CSC were cultured for 48 h, and the relative levels of target proteins and phosphorylation were determined by western blotting. Data are presented as the mean ± SD of the levels of target proteins vs. the β-actin control, or the phosphorylated vs. the total form, from six separate experiments. In addition, Nestinhigh in the presence or absence of LGK974 (1 nM), Nestinlow in the presence or absence of SB216763 (5 uM), and control CSC were tested for their proliferation via mammosphere formation assays. Quantitative analysis of the formed mammospheres. *P <0.05, vs. the Nestin-c or control, except for specifically indicated. CSC, cancer stem cell; SD, standard deviation.
S7096	KY02111 KY02111抑制Wnt信号，促进hPSCs分化为心肌细胞，可能对APC和GSK3β的下游起作用。	Cell Physiol Biochem,2018, 50(2):538-551 Exp Eye Res,2015, 132C:174-178	Transient Wnt inhibition results in persistent decrease of b-catenin. HTM cells were incubated for 4 days in serum-free media, treated with Wnt inhibitors for 8 days in serum free media, and recovered for 4 days in serum-free media before being fixed and stained for b-catenin. (B) HTM cells treated with 10 μM KY02111 or LGK-974 likewise show a reduction of b-catenin staining intensity. (CeD) Quantification of b-catenin staining intensity in HTM cells from 3 donors indicates a statistically significant decrease in intensity after 0.5 μg/mL SFRP1 (SFRP1), 10 μM KY02111, and 10 μM LGK-974. (E) Western blot shows increased T41 phosphorylation of b-catenin after SFRP1 or KY02111 treatment. Data presented as mean ± SEM. Significant difference from control using Tukey's method denoted by * p < 0.05; ***p < 0.001; using Student's T-test denoted by #p < 0.05. n=3. Scale bar 50 μm.
S7085	IWP-2 IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响。IWP-2可特定低抑制 CK1δ。	Biomaterials,2020, 249:120015 Cell Stem Cell,2019, 24(3):447-461.e8. Nat Neurosci,2019, 22(3):484-491	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
S7301	IWP-L6 IWP-L6是高效强效的Porcn的抑制剂，EC50为0.5 nM。
S3842	Isoquercitrin Isoquercitrin, a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation.
S8429	PNU-74654 PNU-75654通过抑制β-catenin和Tcf4的相互作用（Kd=450 nM）,破坏Wnt signaling pathway。	Cell Death Differ,2020, 7 Br J Cancer,2020, 122(4):578-589 Free Radic Res,2019, 53(8):851-864
S7954	CP21R7 (CP21) CP21R7（CP21）是一种有效的、选择性的GSK-3β抑制剂，能有效激活经典Wnt信号通路。	Front Cell Dev Biol,2020, 15;8:309 Biochem Biophys Res Commun,2020, 4;526(3):764-771 Hum Cell,2020, 29
S8129	Salinomycin (from Streptomyces albus) Salinomycin, 曾经被用作抗球虫药，具有抗癌和抗肿瘤干细胞的效果。	Biomed Pharmacother,2020, 16;127:110225 Prostate,2020, 80(3):267-273 EMBO Mol Med,2019, 11(10):e9930	The salinomycin inhibited the growth of CNE-2 in time- and dose-dependent manner. SAL salinomycin
S8761	Adavivint (SM04690) SM04690是一种有效的经典Wnt信号通路抑制剂，抑制TCF/LEF报告基因的EC50为19.5 nM。在多种细胞实验中，它比其他已知的Wnt抑制剂更有效。
S7484	FH535 FH535是一种Wnt/β-catenin信号传导抑制剂，同时也是PPARγ和PPARδ的双重拮抗剂。	Gastroenterology,2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc,2019, 3(7):1246-1260 Gene,2019, 684:95-103	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
S8645	IWP-O1 IWP-O1是porcn抑制剂，在培养细胞中进行的Wnt信号报告基因实验中，EC50为80 pM。它能有效地抑制Hela细胞中Dvl2/3的磷酸化。
S8474	LF3 LF3是一种特异的、对经典Wnt信号通路抑制剂，通过破坏β-catenin和Tcf4的相互作用发挥抑制作用，IC50<2 μM。	FASEB J,2020, 2 Nat Cell Biol,2019, 21(5):627-639 Carcinogenesis,2019, 10.1093/carcin/bgz079
S7490	WIKI4 WIKI4 是新型的Tankyrase抑制剂，作用于TNKS2的IC50为15 nM ,且对Wnt/ß-catenin信号通路也有抑制作用。	Nat Commun,2019, 10(1):4363
S9416	Triptonide Triptonide, isolated from the roots of Tripterygium wilfordii, can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It is also an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent.
S8644	GNF-6231 GNF-6231是一种有效的、具有口服活性的、选择性的Porcupine抑制剂，其IC50为0.8 nM。
S8248	IQ-1 IQ-1可以使小鼠胚胎干细胞在Wnt/β-catenin信号的驱使下扩增并阻止其非定向分化。在经Wnt3a处理的细胞中，维持维持胚胎干细胞(ESC)多能性、阻止PP2A/Nkd的相互作用。	Cell Mol Life Sci,2019, 76(14):2817-2832
S8327	KYA1797K KYA1797K是一种有效的、高度选择性的Wnt/β-catenin抑制剂，在TOPflash实验中，IC50为0.75 μM。	Cell Div,2020, 1;15:2 J Cell Biochem,2020, 121(2):1250-1259 J Immunol,2019, 203(10):2630-2643	A549 cells were treated with KYA1797K for 72 h, cells lysates were collected for western blotting, concentration gradient (1, 12.5 μM, 25 μM) was set for the analysis

目录号	产品描述	文献引用	实验数据
S2924	CHIR-99021 (CT99021) HCl CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂，IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。	Cell, 2020, 30;181(3):621-636 Cell Res, 2020, 30(1):21-33 Nat Commun, 2020, 22;11(1):2585	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1263	CHIR-99021 (CT99021) CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。CHIR-99021 可作为Wnt/β-catenin的激活剂并诱导自噬。	Cell, 2020, 30;181(3):621-636.e22. Cell, 2020, 30;181(3):621-636 Nat Genet, 2020, 52(3):264-272	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S3630	Methyl Vanillate Methyl Vanillate是枳椇子成分之一，在体外能激活Wnt/β-catenin信号通路并诱导成骨分化。
S7914	Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9)是一种成体神经发生的合成促进剂，通过引起成熟神经干细胞/前体细胞(NSPCs)的神经元分化而发挥作用。Isoxazole 9 (Isx-9) 可激活多条信号通路，包括 TGF-β 诱导的上皮-间质转化信号通路 (EMT) ，以及在心脏分化不同阶段的经典和非经典的 Wnt 信号通路。
S8178	Wnt agonist 1 Wnt agonist 1是具有细胞透性的Wnt信号通路激活剂，诱导依赖于β-catenin-和TCF-的转录活性，EC50为0.7 μM。	J Cell Physiol, 2020, 10.1002/jcp.29550 Gut Microbes, 2020, 10.1080/19490976 EBioMedicine, 2019, 45:181-191	Both Wnt sinaling activators of agonist and recombinant protein, and therapeutic agents of fluorouracil and docetaxel stimulated TCF-4 promoter functions of wild-type (wt) could be blocked by Nano-Let-7b, compared with negative control group of mutant-type (mut). In detail, Let-7b alone affected the TCF-4 promoter activity effectively, and wnt signaling activators of either Wnt agonist-1 or Wnt protein attenuated the Let-7b functions significantly. Combined usage of therapeutic agent of either fluorouracil or docetaxel with Let-7b increased the TCF-4 activity when compared to groups treated with Let-7b alone, however, the TCF-4 activity when applying combination was still significantly lower than that of controlled group

目录号	产品描述	文献引用	实验数据
S8647	iCRT3 iCRT3是Wnt/β-catenin信号的拮抗剂，在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。	PLoS One, 2017, 12(7):e0180897

目录号

产品描述

文献引用

实验数据

S8647

iCRT3

iCRT3是Wnt/β-catenin信号的拮抗剂，在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。

PLoS One, 2017, 12(7):e0180897

目录号	产品描述	文献引用	实验数据
S5815	WAY-316606 WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。
S8320	SKL2001 SKL2001是一种新型的Wnt/β-catenin信号通路的激动剂，破坏Axin/β-catenin的相互作用。	Eur Rev Med Pharmacol Sci, 2020, 24(10):5249-5258 J Cell Biochem, 2020, 10.1002 J Cell Mol Med, 2019, 23(10):7088-7098	Western blots of nuclear and cytoplasmic fractions of β-catenin and total CDH3. d The ratio of nuclear/cytosolic of β-catenin was calculated by densitometry analysis.

目录号

产品描述

文献引用

实验数据

S5815

WAY-316606

WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。

S8320

SKL2001

SKL2001是一种新型的Wnt/β-catenin信号通路的激动剂，破坏Axin/β-catenin的相互作用。

Eur Rev Med Pharmacol Sci, 2020, 24(10):5249-5258

J Cell Biochem, 2020, 10.1002

J Cell Mol Med, 2019, 23(10):7088-7098

目录号	产品描述	文献引用	实验数据
S2431^New	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) 可以通过降低肝脏指数来降低鸡的生长性能，而肾脏，心脏和脾脏指数均有增加。TMTD (Tetramethylthiuram disulfide) 通过改变 VEGF，HIF-1α 和 WNT4 的表达来诱发胫骨软骨发育不良 tibial dyschondrolplasia (TD)。TMTD (Tetramethylthiuram disulfide) 广泛应用于橡胶加工中作为低温硫化的超促进剂，且是农业生产中一种重要的农药。

目录号

产品描述

文献引用

实验数据

S2431^New

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) 可以通过降低肝脏指数来降低鸡的生长性能，而肾脏，心脏和脾脏指数均有增加。TMTD (Tetramethylthiuram disulfide) 通过改变 VEGF，HIF-1α 和 WNT4 的表达来诱发胫骨软骨发育不良 tibial dyschondrolplasia (TD)。TMTD (Tetramethylthiuram disulfide) 广泛应用于橡胶加工中作为低温硫化的超促进剂，且是农业生产中一种重要的农药。

研究领域

产品类型

Wnt/beta-catenin

信号通路图

研究领域

抑制剂选择性比较

Wnt/beta-catenin产品