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
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1180 |
XAV-939XAV-939 (NVP-XAV939) 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。 |
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.
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| S2662 |
ICG-001ICG-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。 |
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.
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| S2788 |
Capmatinib (INCB28060)Capmatinib (INCB28060, INC280, NVP-INC280)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。 |
(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). |
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| S7086 |
IWR-1-endoIWR-1-endo (endo-IWR 1)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。 |
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).
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| E0033New |
IWP-4IWP-4 是一种有效的 Wnt/β-catenin 信号通路抑制剂，IC50 为 25 nM。 |
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| S7096 |
KY02111KY02111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。 |
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. |
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| S7085 |
IWP-2IWP-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。 |
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.
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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| S5554 |
Lanatoside CLanatoside C 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。 |
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| S6898 |
RCM-1RCM-1 是一种 Forkhead box M1 (FOXM1) 的无毒抑制剂，可抑制杯状细胞化生并阻止暴露在过敏原中的小鼠体内的 IL-13 和 STAT6 的信号转导。RCM-1 可减少了癌变和核 β-catenin。 |
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| S3842 |
IsoquercitrinIsoquercitrin (Hirsutrin, 3-Glucosylquercetin, Quercetin 3-o-glucopyranoside), 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. |
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| S7981 |
CCT251545CCT251545 是一种有效的口服生物利用型的 WNT 信号抑制剂，在7dF3细胞中的IC50值为5 nM。CCT251545 还可作为选择性化学探针，探讨 CDK8 和 CDK19 在人类疾病中的作用。 |
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| S8429 |
PNU-74654PNU-75654通过抑制β-catenin和Tcf4的相互作用（Kd=450 nM）,破坏Wnt signaling pathway。 |
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| S8129 |
Salinomycin (from Streptomyces albus)Salinomycin (Coxistac, Bio-cox, Procoxacin), 曾经被用作抗球虫药，具有抗癌和抗肿瘤干细胞的效果。 |
The salinomycin inhibited the growth of CNE-2 in time- and dose-dependent manner. SAL salinomycin
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| S8761 |
Adavivint (SM04690)Adavivint (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。 |
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| S8392 |
NCB-0846NCB-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, MAP4K7)的IC50为21 nM。 |
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| S7484 |
FH535FH535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。 |
Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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| S8474 |
LF3LF3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。 |
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| S8968 |
PRI-724PRI-724 (C-82 prodrug, ICG-001 analog) 是一种有效的特异性抑制剂，可破坏 β-catenin 和 CBP 的相互作用。 |
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| S7490 |
WIKI4WIKI4 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。 |
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| S9416 |
TriptonideTriptonide, 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. |
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| S6901 |
MSABMSAB 是一种选择性的 Wnt/β-catenin 信号传导的抑制剂，可与β-catenin结合，促进其降解，特别是下调 Wnt/β-catenin 的靶基因。MSAB 具有有效的抗肿瘤作用。 |
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| S8248 |
IQ-1IQ-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。 |
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| S8327 |
KYA1797KKYA1797K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。 |
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
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| S6745 |
JW55JW55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。 |
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| S8704 |
iCRT14iCRT14是β-catenin/Tcf抑制剂，在HFP实验中Ki值为54 ± 5.2 μM。 |
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| S2924 |
CHIR-99021 (CT99021) HClCHIR-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。 |
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.
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| E0072New |
Indirubin-3′-oximeIndirubin-3'-oxime (IDR3O, I3O) 是一种靛玉红类似物，对 GSK-3β 和 CDK 具有良好的抑制活性。Indirubin-3'-oxime 还抑制 JNKs，对 JNK1、JNK2 和 JNK3 的 IC50 分别为 0.8 μM、1.4 μM 和 1.0 μM。Indirubin-3′-oxime 激活 Wnt/β-catenin 信号并抑制脂肪细胞分化和肥胖。 |
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| S6085New |
KY19382 (A3051)KY19382 (A3051) 是一种 Wnt/β-catenin 信号激活剂，可抑制 CXXC5–DVL 相互作用和 GSK3β 活性，IC50 分别为 19 nM 和 10 nM。 |
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| 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。 |
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. |
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| S3223 |
L-QuebrachitolL-Quebrachitol (L-QCT) 是可从许多植物中分离出来的天然产物，促进增殖和细胞DNA合成。L-Quebrachitol 可上调 bone morphogenetic protein-2 (BMP-2)、runt-related transcription factor-2 (Runx2) 和 mitogen-activated protein kinase (MAPK) 相关调控基因和 Wnt/β-catenin 信号通路，同时下调 nuclear factor-κB(NF-κB) 配体 (RANKL) 受体激活剂的mRNA水平。 |
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| S3630 |
Methyl VanillateMethyl 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。 |
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| 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。 |
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| S7421 |
CGP 57380CGP 57380 是强效的MNK1抑制剂，其IC50为 2.2 μM,对 p38, JNK1, ERK1 和 -2, PKC, 或 c-Src-like kinases显示无抑制活性。CGP 57380 可上调 β-catenin 并加强辐射诱导的凋亡。 |
PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
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| 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。 |
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| S8178 |
Wnt agonist 1Wnt agonist 1 (BML-284 HCL, AMBMP HCL) 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。 |
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
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| S0733 |
Tegatrabetan (BC-2059)Tegatrabetan (BC2059) 是一种 β-Catenin 的拮抗剂。Tegatrabetan (BC2059) 会破坏β-catenin与scaffold protein transducin β-like 1 (TBL1)的结合以及蛋白酶体降解并降低β-catenin核水平。 |
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| S8647 |
iCRT3iCRT3是Wnt/β-catenin信号的拮抗剂，在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。 |
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| S9828New |
WAY-262611WAY-262611 (BML-WN110, Compound 5) 是一种 beta-catenin (β-Catenin) 的激动剂，可增加骨形成速率，在TCF-荧光素酶测定中的EC50值为0.63 μM。WAY-262611 也是一种 dickkopf 1 (DKK1) 的抑制剂。 |
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| S5815 |
WAY-316606WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。 |
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| S8320 |
SKL2001SKL2001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。 |
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.
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| S5992New |
Heparan SulfateHeparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan) 是HS proteoglycans (HSPGs)的成分，是一种存在于细胞表面的线性多糖。Heparan sulfate 可影响小肠上皮细胞(IECs)与 Wnt 的结合亲和力，从而促进经典Wnt信号的激活并促进小肠隐窝上皮损伤后的再生。 |
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| S2431 |
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。 |
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| S6961 |
Foxy-5Foxy-5 是一种Wnt-5a的模拟六肽，是 WNT 信号通路的调节剂，可用于治疗转移性乳腺癌，前列腺癌和结直肠癌。 |
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| S0458 |
KY1220KY1220 通过靶向 Wnt/β-catenin 通路，使得 β-catenin 和 Ras 的稳定性被破坏，其在HEK293 reporter细胞中的IC50值为2.1 μM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1180 |
XAV-939XAV-939 (NVP-XAV939) 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。 |
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.
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| S2662 |
ICG-001ICG-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。 |
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.
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| S2788 |
Capmatinib (INCB28060)Capmatinib (INCB28060, INC280, NVP-INC280)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。 |
(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). |
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| S7086 |
IWR-1-endoIWR-1-endo (endo-IWR 1)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。 |
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).
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| E0033New |
IWP-4IWP-4 是一种有效的 Wnt/β-catenin 信号通路抑制剂，IC50 为 25 nM。 |
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| S7096 |
KY02111KY02111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。 |
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. |
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| S7085 |
IWP-2IWP-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。 |
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.
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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| S5554 |
Lanatoside CLanatoside C 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。 |
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| S6898 |
RCM-1RCM-1 是一种 Forkhead box M1 (FOXM1) 的无毒抑制剂，可抑制杯状细胞化生并阻止暴露在过敏原中的小鼠体内的 IL-13 和 STAT6 的信号转导。RCM-1 可减少了癌变和核 β-catenin。 |
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| S3842 |
IsoquercitrinIsoquercitrin (Hirsutrin, 3-Glucosylquercetin, Quercetin 3-o-glucopyranoside), 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. |
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| S7981 |
CCT251545CCT251545 是一种有效的口服生物利用型的 WNT 信号抑制剂，在7dF3细胞中的IC50值为5 nM。CCT251545 还可作为选择性化学探针，探讨 CDK8 和 CDK19 在人类疾病中的作用。 |
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| S8429 |
PNU-74654PNU-75654通过抑制β-catenin和Tcf4的相互作用（Kd=450 nM）,破坏Wnt signaling pathway。 |
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| S8129 |
Salinomycin (from Streptomyces albus)Salinomycin (Coxistac, Bio-cox, Procoxacin), 曾经被用作抗球虫药，具有抗癌和抗肿瘤干细胞的效果。 |
The salinomycin inhibited the growth of CNE-2 in time- and dose-dependent manner. SAL salinomycin
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| S8761 |
Adavivint (SM04690)Adavivint (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。 |
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| S8392 |
NCB-0846NCB-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, MAP4K7)的IC50为21 nM。 |
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| S7484 |
FH535FH535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。 |
Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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| S8474 |
LF3LF3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。 |
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| S8968 |
PRI-724PRI-724 (C-82 prodrug, ICG-001 analog) 是一种有效的特异性抑制剂，可破坏 β-catenin 和 CBP 的相互作用。 |
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| S7490 |
WIKI4WIKI4 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。 |
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| S9416 |
TriptonideTriptonide, 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. |
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| S6901 |
MSABMSAB 是一种选择性的 Wnt/β-catenin 信号传导的抑制剂，可与β-catenin结合，促进其降解，特别是下调 Wnt/β-catenin 的靶基因。MSAB 具有有效的抗肿瘤作用。 |
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| S8248 |
IQ-1IQ-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。 |
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| S8327 |
KYA1797KKYA1797K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。 |
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
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| S6745 |
JW55JW55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。 |
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| S8704 |
iCRT14iCRT14是β-catenin/Tcf抑制剂，在HFP实验中Ki值为54 ± 5.2 μM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2924 |
CHIR-99021 (CT99021) HClCHIR-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。 |
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.
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| E0072New |
Indirubin-3′-oximeIndirubin-3'-oxime (IDR3O, I3O) 是一种靛玉红类似物，对 GSK-3β 和 CDK 具有良好的抑制活性。Indirubin-3'-oxime 还抑制 JNKs，对 JNK1、JNK2 和 JNK3 的 IC50 分别为 0.8 μM、1.4 μM 和 1.0 μM。Indirubin-3′-oxime 激活 Wnt/β-catenin 信号并抑制脂肪细胞分化和肥胖。 |
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| S6085New |
KY19382 (A3051)KY19382 (A3051) 是一种 Wnt/β-catenin 信号激活剂，可抑制 CXXC5–DVL 相互作用和 GSK3β 活性，IC50 分别为 19 nM 和 10 nM。 |
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| 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。 |
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. |
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| S3223 |
L-QuebrachitolL-Quebrachitol (L-QCT) 是可从许多植物中分离出来的天然产物，促进增殖和细胞DNA合成。L-Quebrachitol 可上调 bone morphogenetic protein-2 (BMP-2)、runt-related transcription factor-2 (Runx2) 和 mitogen-activated protein kinase (MAPK) 相关调控基因和 Wnt/β-catenin 信号通路，同时下调 nuclear factor-κB(NF-κB) 配体 (RANKL) 受体激活剂的mRNA水平。 |
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| S3630 |
Methyl VanillateMethyl 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。 |
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| 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。 |
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| S7421 |
CGP 57380CGP 57380 是强效的MNK1抑制剂，其IC50为 2.2 μM,对 p38, JNK1, ERK1 和 -2, PKC, 或 c-Src-like kinases显示无抑制活性。CGP 57380 可上调 β-catenin 并加强辐射诱导的凋亡。 |
PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
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| 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。 |
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| S8178 |
Wnt agonist 1Wnt agonist 1 (BML-284 HCL, AMBMP HCL) 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。 |
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
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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0733 |
Tegatrabetan (BC-2059)Tegatrabetan (BC2059) 是一种 β-Catenin 的拮抗剂。Tegatrabetan (BC2059) 会破坏β-catenin与scaffold protein transducin β-like 1 (TBL1)的结合以及蛋白酶体降解并降低β-catenin核水平。 |
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| S8647 |
iCRT3iCRT3是Wnt/β-catenin信号的拮抗剂，在Wnt responsive STF16-luc reporter assays中IC50为8.2 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S9828New |
WAY-262611WAY-262611 (BML-WN110, Compound 5) 是一种 beta-catenin (β-Catenin) 的激动剂，可增加骨形成速率，在TCF-荧光素酶测定中的EC50值为0.63 μM。WAY-262611 也是一种 dickkopf 1 (DKK1) 的抑制剂。 |
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| S5815 |
WAY-316606WAY-316606是特异性SFRP1拮抗剂，在人类毛球中激活经典Wnt/β-catenin信号。 |
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| S8320 |
SKL2001SKL2001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。 |
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.
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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5992New |
Heparan SulfateHeparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan) 是HS proteoglycans (HSPGs)的成分，是一种存在于细胞表面的线性多糖。Heparan sulfate 可影响小肠上皮细胞(IECs)与 Wnt 的结合亲和力，从而促进经典Wnt信号的激活并促进小肠隐窝上皮损伤后的再生。 |
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| S2431 |
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。 |
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| S6961 |
Foxy-5Foxy-5 是一种Wnt-5a的模拟六肽，是 WNT 信号通路的调节剂，可用于治疗转移性乳腺癌，前列腺癌和结直肠癌。 |
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| S0458 |
KY1220KY1220 通过靶向 Wnt/β-catenin 通路，使得 β-catenin 和 Ras 的稳定性被破坏，其在HEK293 reporter细胞中的IC50值为2.1 μM。 |
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