Powder: -20°C for 3 years | In solvent: -80°C for 1 year
APS-2-79 hydrochloride (APS-2-79 HCl) 是一种 KSR 依赖性的MEK 拮抗剂,可与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的KSR2。它与 KSR 结合可将 KSR 处于非活性状态,使其无法再结合 RAF 和激活 MEK,从而阻断 Ras-MAPK 信号通路。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 253 | 现货 | ||
2 mg | ¥ 356 | 现货 | ||
5 mg | ¥ 640 | 现货 | ||
10 mg | ¥ 1,030 | 现货 | ||
25 mg | ¥ 2,560 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,470 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 640 | 现货 |
产品描述 | APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. |
靶点活性 | KSR2:120 nM |
体外活性 | APS-2-79 functions as an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site. APS-2-79 is inactive when KSR was absent or when the KSR2(A690F) mutant was used for in vitro assays. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling[1]. |
激酶实验 | JNK phosphorylation: 500,000 cells/well are seeded in 6-well plates and incubated overnight. Cells are then incubated for 1 h with test compounds or DMSO as vehicle control (?nal concentration 1% v/v). Puromycin is added (?nal concentration of 18 μM) and cells incubated for a further 10 min to label nascent polypeptide chains. Background labelling is determined by incubating cells without puromycin. Cells are then washed in HBSS, harvested by scraping and centrifuged (300 g, 5 min). Cells are resuspended in 0.5 mL 50 mM DTT containing phosphatase inhibitors and incubated at 95℃ for 10 min. Samples are then snap frozen in liquid nitrogen and stored at -20℃ until blotted. Samples (20–30 μg protein/sample) are blotted onto a PVDF membrane. The membrane is blocked and incubated with anti-phospho-Thr183/Tyr185-JNK antibody overnight at 4℃. Secondary antibodies are used to label the primary antibody and detected using an infrared scanner. The intensity of the ?uorescence signal for anti-phospho-JNK antibody is background corrected and normalized for loading. |
细胞实验 | Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the timecourse of assays. Specifically, A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors for 72hrs. Cell viability is measured using resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls(Only for Reference) |
别名 | APS-2-79 HCl, APS-2-79 |
分子量 | 423.89 |
分子式 | C23H21N3O3·HCl |
CAS No. | 2002381-31-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 90 mg/mL (212.3 mM)
Ethanol: 30 mg/mL (70.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.3591 mL | 11.7955 mL | 23.591 mL | 58.9776 mL |
5 mM | 0.4718 mL | 2.3591 mL | 4.7182 mL | 11.7955 mL | |
10 mM | 0.2359 mL | 1.1796 mL | 2.3591 mL | 5.8978 mL | |
20 mM | 0.118 mL | 0.5898 mL | 1.1796 mL | 2.9489 mL | |
50 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1796 mL | |
DMSO | 100 mM | 0.0236 mL | 0.118 mL | 0.2359 mL | 0.5898 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。
APS-2-79 hydrochloride 2002381-31-7 MAPK MEK MAP2K APS-2-79 HCl APS-2-79 MAPKK Inhibitor Mitogen-activated protein kinase kinase APS 2 79 hydrochloride APS279 hydrochloride inhibit APS-2-79 Hydrochloride inhibitor