NCB-0846
产品说明书
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同义名 : | - |
| CAS号 : | 1792999-26-8 | |
| 货号 : | A358703 | |
| 分子式 : | C21H21N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 375.424 | |
| MDL号 : | MFCD30749187 | |
| 存储条件： |
Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(79.91 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Wnt signaling plays important roles in carcinogenesis and embryonic development. TNIK is a serine/threonine kinase that functions as an activator of the Wnt signaling pathway. TNIK is recruited to promoters of Wnt target genes and required to activate their expression. TCF4 is a substrate of the TNIK enzyme. TNIK phosphorylates TCF4 and regulates its transcriptional activity. TNIK together with NEDD4 and RAP2A form a signaling complex which regulates neuronal dendrite extension and arborization during development. TNIK may also play a role in cytoskeletal rearrangements and regulate cell spreading[3]. NCB-0846 is a TNIK inhibitor. The inhibitory IC50 of NCB-0846 against TNIK kinase was 21 nM[4]. In an experiment system of recombinant TCF4 and TNIK proteins, NCB-0846 induced faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1 - 0.3 μM and completely inhibited the phosphorylation of TCF4 at a concentration of 3 μM . Furthermore, NCB-0846 blocked the autophosphorylation of TNIK in hct116 cells. At the concentrations of 3 μM or 10 μM, NCB-0846 reduced the expression of the Wnt target genes AXIN2 and MYC as well as that of TNIK in hct116 cells. NCB-0846 also reduced the expression of TNIK, AXIN2 and cMYC at the protein level at the concentration range of 1 – 10 μM in hct116 and DLD-1 cells[4]. According to another report, NCB-0846 at the concentrations of 1 μM or 3 μM reduced colony formation of cells derived from patients of prostate cancer[5]. In a hct116 xenograft model established in balb/c nude mice, NCB-0846 was administrated to the mice orally at the doses of 40 mg/kg or 80 mg/kg bid. Both doses of NCB-0846 suppressed tumor growth[4]. In a Wnt-driven tumorigenesis model utilizing Apcmin/+ mice, 3 doses of NCB-0846, including 22.5 mg/kg, 45 mg/kg, 90 mg/kg were administrated. NCB-0846 dose dependently reduced the multiplicity and dimensions of tumours that developed in the small intestine of mice[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.66mL 0.53mL 0.27mL |
13.32mL 2.66mL 1.33mL |
26.64mL 5.33mL 2.66mL |
| 参考文献 |
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