化合物FMK TQ0310
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 821794-92-7 | ¥4,590.00 | 询底价 |
1 mL | 821794-92-7 | ¥1,880.00 | 询底价 |
10 mg | 821794-92-7 | ¥2,770.00 | 询底价 |
1 mg | 821794-92-7 | ¥655.00 | 询底价 |
2 mg | 821794-92-7 | ¥957.00 | 询底价 |
50 mg | 821794-92-7 | ¥6,580.00 | 询底价 |
5 mg | 821794-92-7 | ¥1,830.00 | 询底价 |
500 mg | 821794-92-7 | ¥17,900.00 | 询底价 |
100 mg | 821794-92-7 | ¥8,960.00 | 询底价 |
Product Introduction
Bioactivity
英文名: FMK
描述: FMK 是一种不可逆的 RSK2 抑制剂,能够共价修饰 RSK 的 C 末端区域。
细胞实验: RSK2 expressing Ba/F3 cell lines are generated by retroviral transduction as described by using Ba/F3 cells stably expressing FGFR3 TDII with pMSCV-puro plasmids encoding myc-tagged RSK2 variants, followed by antibiotic selection. For cell viability assays, 1×10^5 Ba/F3 cells stably expressing FGFR3 are cultured in 24-well plates with media containing increasing concentrations of FMK, acidic FGF (10 nM), and heparin (30 μg/mL) in the absence of IL-3. The relative cell viability at each experimental time point is determined by using the Celltiter96AQueous One solution proliferation kit [3].
激酶实验: To determine the ability of FGFR3 to phosphorylate RSK2, 500 ng of purified recombinant RSK2 variants are incubated with 500 ng of recombinant active FGFR3 in 10 mM HEPES (pH 7.5), 150 mM NaCl, 1 mM DTT, 0.01% Triton-X-100, 10 mM MnCl2, and 200 μM ATP for 30 min at 30°C. Phosphorylation of Y529 RSK2 is detected by specific phospho-antibody. To determine kinase activity of RSK2 CTD variants, purified recombinant RSK2 CTD proteins (500 nM) are incubated with 500 nM of active ERK in 20 mM HEPES [pH 8.0], 10 mM MgCl2, 2 mM tris-(2-carboxyethyl)-phosphine (TCEP), and 200 μM ATP for 1 hr at 30°C. Kinase reactions are initiated by the addition of 5 μCi of [γ-32P] ATP and 100 μM peptide substrate (CTD-tide), followed by incubation for 20 min at room temperature. Kinase activity is determined using the standard disk phospho-cellulose assay [3].
体外活性: The pretreatment of ARVMs with 3 μM FMK attenuates the increase in Ser386 phosphorylation, but it has no inhibitory effect on the increase in Thr577 phosphorylation [1]. FMK inhibits relatively few protein kinases in the panel, although it does inhibit protein tyrosine kinases, such as Src, Lck, Yes and Eph-A2, as well as S6K1. FMK will not inhibit RSK if the N-terminal kinase domain is activated by a mechanism that is independent of the C-terminal domain[2]. Fmk potently inactivates the CTD auto-kinase activity of RSK1 and RSK2 with high specificity in mammalian cells. Targeting RSK2 by FMK attenuates FGFR3-induced cytokine-independent growth in Ba/F3 cells. FMK inhibits cytokine-independent proliferation of Ba/F3 cells conferred by FGFR3 [3].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : Insoluble
DMSO : 90 mg/mL (262.9 mM)
关键字: FMK
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途