生物试剂
>
生化试剂
>
信号通路
> JNJ-47117096 hydrochloride
加入收藏 取消收藏

JNJ-47117096 hydrochloride  ≥98%

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

件 库存{{model.attbuying.number}}件
立即购买 加入购物车 下载说明书

看了又看
包装规格：1mg 5mg 10mg 100mg in glass bottle
溶解性：溶于DMSO（≥250mg/mL）
产品描述：基本信息 产品编号：J10065 产品名称：JNJ-47117096 hydrochloride CAS: 1610536-69-0   储存条件 粉末 -20℃ 四年     分子式： C21H23ClN4O2 溶于液体 -80℃ 六个月 分子量 398.89 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5070mL 12.5348mL 25.0696mL 5mM 0.5014mL 2.5070mL 5.0139mL 10mM 0.2507mL 1.2535mL 2.5070mL   生物活性 产品描述 一种有效的，选择性的 MELK 抑制剂，IC50 值为 23nM；同时对 Flt3 的作用较强，IC50 值为 18nM。 靶点/IC50 IC50: 23nM (MELK), 18nM (Flt3) 体外研究 JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23nM, also effectively inhibits Flt3, with an IC50 of 18nM, and slighitly blocks CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC50, 810nM, 760nM, 1000nM, 1000nM).JNJ47117096 (MELK-T1) suppresses the proliferation of Flt3-driven Ba/F3 cell lines, with an IC50 of 1.5μM in the absence of IL-3,while no inhibitory activity is observed in the presence of IL-3. JNJ-47117096 does not inhibit the proliferation of Ba/F3 cell lines transfected with either FGFR1, FGFR3, or KDR, either in the presence or absence of IL-3.JNJ-47117096 (MELK-T1, 10 μM) delays the progression of MCF-7 cells through S-phase. JNJ-47117096 inhibits MELK, and then exerts stalled replication forks and DNA double-strand breaks (DSBs). JNJ-47117096 activates the ATM-mediated DNA-damage response (DDR). JNJ47117096 (3, 10μM) results in a growth arrest and a senescen phenotype.Moreover, JNJ-47117096 induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.       推荐实验方法(仅供参考) 激酶实验： Inhibition of MELK kinase activity is measured using a radioactive filter binding assay. Briefly, each assay well contains 1.25nM MELK (human, residues 1-340) 10μM ATP, 6.7 uCi/mL γ 33P-ATP, 3μM biotinylated ZIP-tide peptide (BiotinKKLNRTLSFAEPG) in 30μL reaction buffer (25mM Tris pH 7.5,10mM MgCl2, 1mM DTT, 1mM EGTA, 0.1% Triton X100). Kinase reactions are performed for 25 minutes at room temperature before stopping with 40μL 2% orthophosphoric acid. Unbound radioactivity is removed by filtering the reaction through a MAPH filter plate. The trapped 33P labelled peptide is then washed twice with 200μL 0.5% orthophosphoric acid, 2μL Microscint-20 added per well and the amount of radioactivity determined by scintillation counting using a Topcount. To calculate compound IC50, semi-log serial dilutions are used to produce 8-point dose-response curves in duplicate. IC50 values are then derived using the four parameter logistic fit method in GraphPad Prism 5.0.   细胞实验:   Compounds (JNJ-47117096) dissolved in DMSO are sprayed into 384-well plates (100nL/well). A suspension of Ba/F3-Flt3 cells is added (20,000 cell/well), followed by the addition of 10ng/mL IL3. The cells are incubated for 24 h at 37℃ and 5% CO 2. Alamar Blue solution is added, and after 4h incubation at 37℃, the fluorescent intensity is measured on a Fluorescence plate reader (540nm excitation and 590 nm emission). The control experiment in the absence of IL3 is performed in the same way. To calculate compound IC50, semi-log serial dilutions are used to produce 8- point dose-response curves in duplicate. A best-fit curve is fitted by a minimum sum of squares method to the plot of %Control vs. compound concentration. From this an IC50 value is calculated.
保存条件：-20℃

猜你喜欢