Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KYA1797K 是一种选择性 Wnt/β-catenin 抑制剂(IC50:0.75 µM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,450 | 现货 | ||
50 mg | ¥ 3,680 | 现货 | ||
100 mg | ¥ 5,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 727 | 现货 |
产品描述 | KYA1797K is a highly potent and selective inhibitor. Wnt/β-catenin IC50 is 0.75 μM through TOPflash assay. |
靶点活性 | Wnt/β-catenin:0.75 μM |
体外活性 | KYA1797K significantly decreases reporter activities for the Wnt/β-catenin and MAPK/ERK pathways but does not affect the reporter activities of other cancer-related pathways, such as the Notch and TGFβ pathways, thus, KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. KYA1797K enhances the β-catenin binding affinity of endogenous axin, GSK3β and β-TrCP. Interaction between APC and β-catenin is not enhanced by KYA1797K. It promotes the formation of the β-catenin destruction complex. KYA1797K degrades both β-catenin and Ras in these cells(CRC lines SW480, LoVo, DLD1 and HCT15) in a dose-dependent manner, cell proliferation is also suppressed by KYA1797K treatment. KYA1797K inhibits proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. KYA1797K directly targeted axin and modulated conformation of the β-catenin destruction complex[1]. |
体内活性 | KYA1797K administration by intraperitoneally injection(i.p.) (25 mg/kg) reduces both weight and volume of the tumor by 70% in mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations. KYA1797K treatment significantly reduces levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling target. No change in the weight and no abnormalities in liver tissues of mice treated with KYA1797K. KYA1797K significantly reduces the subcellular localization of β-catenin in the nuclei and pan-Ras on the membrane of tumor cells. Thus, KYA1797K has anti-tumor effect[1]. |
细胞实验 | To assay cell proliferation, HCT15 or SW480 cells are plated at a density of 2 × 104 cells/well, and D-WT or D-MT cells were seeded at a density of 1×104 cells/well in a 24-well plate. The cells are then treated with 25 μM KYA1797K or with control (DMSO) for 72 h. In a 96-well plate, cells are seeded at a density of 3 × 103 cells/well. After 24 h, the cells are treated with KY1220, KYA1797K, IWR-1 or XAV939 for 4 d. Next, MTT reagent is added to each well at a concentration of 0.25 mg/ml. After incubation for 2 h at 37°C, insoluble purple formazan is obtained by removing the medium and incubating in 1 ml (24-well) or 200 μl (96-well) of DMSO for 1 h. The absorbance of the formazan product is determined at 590 nm every 24 h. (Only for Reference) |
分子量 | 442.51 |
分子式 | C17H11N2O6S2·K |
CAS No. | 1956356-56-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6 mg/mL (13.56 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2598 mL | 11.2992 mL | 22.5984 mL | 56.4959 mL |
5 mM | 0.452 mL | 2.2598 mL | 4.5197 mL | 11.2992 mL | |
10 mM | 0.226 mL | 1.1299 mL | 2.2598 mL | 5.6496 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KYA1797K 1956356-56-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Wnt Beta catenin β-catenin inhibit Inhibitor KYA-1797K inhibitor