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4°C, sealed storage, away from moisture
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货期：1-2天
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10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2180.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1300.0 |
| 规格： | 10 mg | 产品价格： | ￥1800.0 |
| 规格： | 50 mg | 产品价格： | ￥5400.0 |
| 规格： | 100 mg | 产品价格： | ￥8400.0 |
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TAK-960 dihydrochloride
MCE 国际站：TAK-960 dihydrochloride
产品活性：TAK-960 dihydrochloride 是一种有效的，可口服的，选择性的 polo-like kinase 1 (PLK1) 抑制剂，IC50 为 0.8 nM。TAK-960 dihydrochloride 对 PLK2 和 PLK3 也有抑制作用，IC50 分别为 16.9 和 50.2 nM。TAK-960 dihydrochloride 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。
研究领域：Cell Cycle/DNA Damage
作用靶点：Polo-like Kinase (PLK)
In Vitro: TAK-960 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells.
TAK-960 dihydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.
In Vivo: TAK-960 dihydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.
In animal models, TAK-960 dihydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts.
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Metabolism 上在线发表了题为 Tripartite motif 16 ameliorates nonalcoholic steatohepatitis by promoting the degradation of phospho-TAK1 的研究成果 (4)。该研究发现 E3 泛素连接酶 TRIM16 通过促进 p-TAK1 的泛素化依赖性降解，改善 NASH 进展过程中的脂质积累和炎症。 图片来源：Cell Metabolism研究内容肝细胞的脂肪毒性诱导 TRIM16 的表达脂肪毒性是脂质过度积累
Smads, TAK1, and Their Common Target ATF-2 Play a Critical Role in Cardiomyocyte Differentiation We previously demonstrated that bone morphogenetic proteins (BMPs) induce cardiomyocyte differentiation through the mitogen-activated protein kinase
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can be used:Quinine dihydrochloride 20 mg salt/kg base given I.V. in 5% w/v dextrose or normal saline as a once-only 4 hour infusion followed, 4 hours later, by quinine dihydrochloride 10 mg salt/kg base 4-hour infusions 8 hourly.Where a syringe pump
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