Wnt/beta-catenin
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1180 | XAV-939 | <1 mg/mL | 12 mg/mL | <1 mg/mL |
| S2662 | ICG-001 | <1 mg/mL | 100 mg/mL | 10 mg/mL |
| S7086 | IWR-1-endo | <1 mg/mL | 21 mg/mL | <1 mg/mL |
| S7037 | Wnt-C59 (C59) | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S7143 | LGK-974 | <1 mg/mL | 79 mg/mL | <1 mg/mL |
| S8761 | Adavivint (SM04690) | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S9416 | Triptonide | -1 mg/mL | 71 mg/mL | -1 mg/mL |
| S8645 | IWP-O1 | <1 mg/mL | 86 mg/mL | 86 mg/mL |
| S7096 | KY02111 | <1 mg/mL | 75 mg/mL | <1 mg/mL |
| S7085 | IWP-2 | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S7301 | IWP-L6 | <1 mg/mL | 25 mg/mL | <1 mg/mL |
| S3842 | Isoquercitrin | -1 mg/mL | 92 mg/mL | -1 mg/mL |
| S8429 | PNU-74654 | <1 mg/mL | 64 mg/mL | 10 mg/mL |
| S7954 | CP21R7 (CP21) | <1 mg/mL | 63 mg/mL | 1 mg/mL |
| S8129 | Salinomycin (from Streptomyces albus) | <1 mg/mL | 100 mg/mL | 79 mg/mL |
| S7484 | FH535 | <1 mg/mL | 72 mg/mL | <1 mg/mL |
| S8474 | LF3 | <1 mg/mL | 83 mg/mL | 5 mg/mL |
| S7490 | WIKI4 | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S8262 | PRI-724 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8644 | GNF-6231 | <1 mg/mL | 89 mg/mL | 5 mg/mL |
| S8248 | IQ-1 | <1 mg/mL | 72 mg/mL | 7 mg/mL |
| S8327 | KYA1797K | <1 mg/mL | 7.2 mg/mL | <1 mg/mL |
| S3630 | Methyl Vanillate | 12 mg/mL | 36 mg/mL | 36 mg/mL |
| S8178 | Wnt agonist 1 | <1 mg/mL | 77 mg/mL | <1 mg/mL |
| S5815 | WAY-316606 | <1 mg/mL | 90 mg/mL | 7 mg/mL |
| S8647 | iCRT3 | <1 mg/mL | 78 mg/mL | 78 mg/mL |
| S8320 | SKL2001 | <1 mg/mL | 57 mg/mL | 57 mg/mL |
- Wnt/beta-catenin抑制剂（27）
- 新Wnt/beta-catenin产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1180 |
XAV-939XAV-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。 |
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。 |
Immunocytochemical analysis of SOX1 (a–d), SOX2 (e–h) and SOX3 (i–l) expression in NT2/D1 cells treated with either DMSO (a, b, e, f, i, j) or ICG-001 (c, d, g, h, k, l). Cell nuclei were stained with DAPI (b, d, f, h, j, l). Scale bar 50 μm.
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| S7086 |
IWR-1-endoIWR-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。 |
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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| 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。 |
In vitro treatment with C59 (Wnt-i) decreased the active (non-phosphorylated) β-catenin level in Eed cKO primary rib chondrocytes. Chondrocytes were cultured for 24 h in the presence of C59 (Wnt-i).
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| S7143 |
LGK-974LGK-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。 |
(c) Immunohistochemical images of intestinal sections from E-Rspo2 and R26-rtTA/P-Rspo3 mice treated with either DMSO or LGK974. BrdU was stained for proliferation. Scale bars, 100 μm.
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| S8761New |
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。 |
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| S9416New |
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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| S8645New |
IWP-O1IWP-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。 |
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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。 |
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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| S7301 |
IWP-L6IWP-L6是高效强效的Porcn的抑制剂，EC50为0.5 nM。 |
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| S3842 |
IsoquercitrinIsoquercitrin, 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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| 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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| 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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| 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。 |
The salinomycin inhibited the growth of CNE-2 in time- and dose-dependent manner. SAL salinomycin
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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。 |
BrdU assay was used to detect the proliferation level of cells in four groups: the control group, FH535 (15 μM) group, NAM (50 mM) + FH535 (15 μM) group, REV (100 μM) + FH535 (15 μM) group. A. At the next day, the cells were fixed and immunostained for BrdU (red) and with DAPI (blue) then merged the two pictures of the same field. The scale bar is 100 μm. B. The total numbers of cells (DAPI-staining cells) per field in the four groups. C. BrdU-positive rate of C2C12 cells was analyzed. Each value represents the mean ± standard error of the mean of triplicate determinations from three independent cell preparations. *P<0.05, **P<0.01, ***P<0.001 vs the value of the control; n=3; error bars ± standard error of means. Statistical analysis was conducted using one-way ANOVA. Original magnification is ×200.
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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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| 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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| S8262 |
PRI-724在肿瘤干细胞中，PRI-724是有效的经典Wnt信号通路的特异性抑制剂，具有潜在的抗肿瘤活性。PRI-724抑制beta-catenin和其共激活剂CBP的结合与招募。 |
Lpcat3KD 3T3L1 pre-adipocytes were treated with different concentration of Wnt/-catenin pathway inhibitors and then underwent differentiation. The fully differentiated cells were collected. Triglyceride, free cholesterol, and total cholesterol were measured. IWR-1-endo (IC50=180nM) inhibits Wnt-induced stabilization of β-catenin by acting on the target of β-catenin destruction complex in cytosol; PRI-724 (IC50=150 nM) and ICG-001 (IC50=3 μM) inhibit the recruiting of β-catenin with its coactivator element-binding protein(CBP) in nucleus. Values are mean ± SD, n = 3. Bars labeled with different uppercase letters are statistically different (p < 0.05).
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| S8644 |
GNF-6231GNF-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。 |
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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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| 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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| S8178 |
Wnt agonist 1Wnt 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。 |
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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| S5815New |
WAY-316606WAY-316606是特异性SFRP1拮抗剂，在人类毛球中抑制经典Wnt/β-catenin信号。 |
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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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| 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。 |
G. Enforced Wnt signaling by SKL-2001 restored cell growth in miR-520e overexpression A549 cells
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