Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHIR-98014 (CT98014) 是有效的,细胞通透的GSK-3抑制剂,可抑制 GSK-3α (IC50:0.65 nM) 和 GSK-3β (IC50:0.58 nM) 的活性,对 cdc2 和 erk2 的作用较弱。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 292 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 755 | 现货 |
产品描述 | CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo. |
靶点活性 | GSK-3α:0.65 nM, GSK-3β:0.58 nM |
体外活性 | CHIR 98014降低高血糖和改善葡萄糖利用的效果并不限于db/db小鼠和ZDF大鼠,由于观察到ob/ob小鼠,饮食诱导的糖尿病C57BL/6小鼠和用CHIR-2处理的葡萄糖不耐受的SHHF大鼠出现类似结果.此外,CHIR-98014降低了出生后大鼠皮质和海马中tau蛋白的磷酸化(Ser396).GSK-3抑制剂CHIR-98014作用于从瘦弱的患有糖尿病和抗胰岛素的ZDF鼠分离的I型骨骼肌,激活GS活性.瘦弱患有糖尿病鼠分离的肌肉中,胰岛素和CHIR 98014激活的GS比ZDF鼠分离的肌肉中强很多.CHIR 98014或胰岛素作用于这些细胞和肌肉不会改变全部GS活性. 同时,CHIR 98014不会影响从瘦弱动物分离的肌肉中胰岛素剂量反应. |
体内活性 | 虽然CHIR-98014作为ATP结合的简单竞争性抑制剂,但它对GSK-3显示出相对于20种其他蛋白激酶(包括Cdc2,ERK2,Tie-2和KDR在内)500倍至> 1000倍的选择性。CHIR 98014抑制人类GSK-3β,Ki值为0.87 nM。CHIR 98014抑制CDC2,IC50为3.7 μM。然而,CHIR 98014对GSK-3高度同源的ɑ和β亚型具有相似效果,但是在GSK-3和最接近的同系物cdc2和erk2间具有明显区别。CHIR 98014使CHO-IR和鼠肝细胞达到半数最大GS刺激反应的浓度分别为106和107 nM。将表达胰岛素受体的CHO-IR细胞或原代大鼠肝细胞暴露于递增浓度的抑制剂CHIR98014中导致GS活性比率高于基础值的两倍至三倍的刺激。 |
激酶实验 | Kinase assays: Polypropylene 96-well plates are ?lled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing kinase, peptide substrate, and any activators. CHIR-98014 or controls are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a ?nal concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed ?ve times with PBS, ?lled with 200 μL of scintillation ?uid, sealed, left 30 min, and counted in a scintillation counter. All steps are performed at room temperature. |
细胞实验 | CHO-IR cells expressing human insulin receptor are grown to 80% con?uence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 mL of medium without fetal bovine serum. After 24 hours, medium is replaced with 1 mL of serum-free medium containing GSK-3 inhibitor CHIR 98014 or control (?nal DMSO concentration 0.1%) for 30 min at 37 °C. Cells are lysed by freeze/thaw in 50 mM tris (pH 7.8) containing 1 mM EDTA, 1 mM DTT, 100 mM NaF, 1 mM phenylmethylsulfonyl ?uoride, and 25 μg/mL leupeptin (buffer A) and centrifuged 15 min at 4 °C/14000 g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mM glucose-6-phosphate. (Only for Reference) |
别名 | CHIR 98014, CT98014, CHIR98014 |
分子量 | 486.31 |
分子式 | C20H17Cl2N9O2 |
CAS No. | 252935-94-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 8 mg/mL (16.45 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0563 mL | 10.2815 mL | 20.563 mL | 51.4075 mL |
5 mM | 0.4113 mL | 2.0563 mL | 4.1126 mL | 10.2815 mL | |
10 mM | 0.2056 mL | 1.0282 mL | 2.0563 mL | 5.1408 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。
CHIR-98014 252935-94-7 Angiogenesis MAPK PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors FGFR GSK-3 Src S6 Kinase Glycogen synthase kinase-3 CT-98014 CHIR 98014 Inhibitor CT98014 CHIR98014 inhibit CT 98014 Glycogen synthase kinase 3 inhibitor