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- 技术资料
- CAS号：
915759-45-4
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥397.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥167.0 |
| 规格： | 5mg | 产品价格： | ￥358.0 |
| 规格： | 10mg | 产品价格： | ￥566.0 |
| 规格： | 25mg | 产品价格： | ￥1040.0 |
| 规格： | 50mg | 产品价格： | ￥1736.0 |
| 规格： | 100mg | 产品价格： | ￥2528.0 |
Product Introduction
Bioactivity
| 名称 | WAY 316606 |
| 描述 | WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. |
| 细胞实验 | U2OS bone cells are infected with recombinant adenovirus 5 (Ad5)?WNT3 at a multiplicity of infection (MOI) of 2, followed by infection with Ad5-sFRP-1 and Ad5-16xTCF-luciferase, each at an MOI of 10. Four hours after infection, the cells are frozen in sterile cryogenic vials at a cell density of 9×106 cells/mL and stored in a ?150°C freezer. For the assay, a vial of frozen cells is thawed, and the cells are resuspended in plating medium [phenol red-free RPMI 1640 medium containing 5% fetal calf serum, 2 mM GlutaMAX-l, and 1% (v/v) penicillin-streptomycin] to a final cell density of 1.5×105 cells/mL. The resuspended cells are then plated in 96-well tissue culture treated plates at a volume of 100 μL of cell suspension/well (i.e., 1.5×104 cells/well). The plates are incubated at 37°C inside a 5% CO2/ 95% humidified air incubator for 5 h or until the cells have attached and started to spread. Prior to the addition of WAY-316606, the medium is replaced with 50 μL/well of phenol red-free RPMI 1640 containing 10% fetal calf serum, 2 mM GlutaMAX-l, and 1% (v/v) penicillin-streptomycin. WAY-316606, or vehicle (typically DMSO), diluted in phenol red-free RPMI 1640 containing 2 mM GlutaMAX-l, and l % (v/v) penicillin-streptomycin are then added to the wells in replicates of 4 wells/dilution and the plates are incubated at 37°C overnight. Dose?response experiments are performed with the compounds in 2-fold serial dilutions from 10000?4.9 nM. After the overnight incubation, the cells are washed twice with 150 uL/well of PBS w/o calcium or magnesium and lysed with 50 μL/well of 1× cell culture lysis reagent on a shaker at room temperature for 30 min. Aliquots of the cell lysates (30 μL) are transferred to 96-well luminometer plates, and the luciferase activity is measured in a MicroLumat PLUS luminometer using 100 μL/well of a luciferase substrate. |
| 激酶实验 | WAY-316606 binding to purified sFRP is determined by spectroscopy methods. The sFRP-1 or -2 stock solutions are diluted to 1 μM in a buffered solution and the initial fluorescence is measured. Increasing concentrations of WAY-316606 (0 to 50 μM) are added to the protein in the cuvette and incubated for 5 min prior to assessing fluorescence intensity using a Fluoromax-2 fluorometer. In control experiments, the DMSO (vehicle control)-matched buffer solution is used. Fluorescence spectra are scanned in the ratio mode (S/R, signal/reference) to compensate for variations in lamp output as a function of wavelength [2]. |
| 体外活性 | WAY-316606对U2-OS细胞中Wnt-Luciferase活性的EC50值为0.65 μM[1]。WAY-316606以0.08 μM的KD结合到分泌型frizzled相关蛋白(sFRP)-1抑制剂，并以0.65 μM的EC50抑制sFRP-1。同时，WAY-316606也能与sFRP-2结合，但结合能力弱于sFRP-1，其KD值为1 μM。使用一种含有荧光探针化合物的荧光偏振结合实验，并采用竞争结合方式对纯化的人sFRP-1蛋白进行测试，得出WAY-316606的IC50为0.5 μM [2]。 |
| 体内活性 | WAY-316606在新生小鼠颅骨实验中能促进骨骼形成。该化合物以剂量依赖的方式显著增加总骨骼面积，高达60%，其中EC50约为1 nM。WAY-316606具有良好的水溶性、对细胞色素p450酶系（3A4、2D6、2C9）的中度至低度抑制作用，并在大鼠与人类肝微粒体中表现出良好稳定性（每种生物体中半衰期均>60分钟）。在雌性Sprague-Dawley大鼠中，经单次静脉注射给药（2 mg/kg）后，WAY-316606展现出高等于肝脏血流量的血浆清除率（77 mL/min/kg），导致无论给药途径如何，血浆中化合物暴露水平迅速下降[2]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (22.3 mM), Solution. DMSO : 125 mg/mL (278.72 mM), Sonication is recommended. 10% DMSO+90% Saline : < 10 mg/mL (22.3 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | WAY-316606 | WAY316606 | WAY 316606 | sFRP-1 | Secreted frizzled related protein 1 | SARP-2 | Inhibitor | inhibit | FrzA | beta-catenin | betacatenin | bcatenin |
| 相关产品 | Urea | Nimbolide | Bisdemethoxycurcumin | Monensin sodium salt | Neohesperidin | XAV-939 | Isoquercetin | Chlorquinaldol | Methyl Vanillate | (±)-Nornicotine | Ethyl linoleate | Wnt pathway activator 1 |
| 相关库 | Inhibitor Library | Neuroprotective Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Pancreatic Cancer Compound Library | Anti-Alzheimer's Disease Compound Library | Cancer Cell Differentiation Compound Library | Stem Cell Differentiation Compound Library | Anti-Obesity Compound Library | Hematonosis Compound Library | Neuronal Differentiation Compound Library | Reprogramming Compound Library |
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同浓度之间对细胞分化的影响，或不同药物对肿瘤细胞的生存的影响等，此时应采用单因素方差分析（One-way ANOVA）；例如，我们用不同药物处理肿瘤细胞，比较化合物处理后肿瘤细胞的存活率，评价化合物抗肿瘤活性；首先，我们需要将对不同组进行定义，1 表示对照组，2 表示化合物 1 处理组，3 表示化合物 2 处理组，4 表示化合物 3 处理组；而在进行单因素方差分析前我们需要检验方差齐性，步骤同 t 检验中的 F 检验。从 F 检验的结果可看出，p 为 0.001，有显著性差异，说明此时方差不齐。接下
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. adopt在科学领域，adapt 指的是改变或修改某事/物用于另一种用途。例如，「The protocol of Sambrook et al. (1989) was adapted in the following way.」 「用以下方式调整了 Sambrook 等人（1989）的方案。」这意味着对该方案进行了修改，并且将在随后进行描述。adopt 某事/物即录用、接受或遵循计划。例如，「The protocol of Yu et al. (2001) was adopted.」 「采用了 Yu
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化合物 WAY 316606【915759-45-4】
￥167 - 2528
