化合物BQU57 T2267

Product Introduction
Bioactivity


英文名: BQU57

描述: BQU57 能够选择性抑制 Ral，且对 Ral 的选择性高于 Ras、Rho，能够作用于 H2122(IC50:2.0 μM)和 H358(IC50:1.3 μM)。

细胞实验: Growth inhibition on human lung cancer cells by the compounds are measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 mL of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on cell line) after incubation, cells are stained with 1.0 mg/mL Nitro Blue Tetrazolium and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in 50% reduction in colony number compared to DMSO treated control. After 48 hr, cells are subjected to the soft agar colony formation assay. (Only for Reference)

激酶实验: HDAC Enzyme Assay: The commercially availablae human recombinant enzyme and fluorogenic HDAC assay kits have used to measure percent inhibition and IC50 values of three HDAC isozymes (HDAC2, HDAC4, HDAC6). Briefly, the inhibitor is added sequentially to a black, flat-bottom 96-well microtiter plate, and the reaction mixture is incubated for 30 min at 37°C. The potent HDAC inhibitor trichostatin A (included in the assay kit) is added to the bifunctional HDAC assay developer at a final reaction concentration of 1 μM to stop deacetylation and initiate the release of the fluorophore. The reaction mixture is further incubated at room temperature for 15 min. Fluorescence is measured on a Spectra Max Gemini XPS using an excitation wavelength of 360 nm and a detection wavelength of 460 nm.

体外活性: 50 mg/kg,i.p. BQU57在负荷人肺H2122肿瘤的小鼠体内,明显抑制RalA和RalB的活化,并且剂量依赖性抑制肿瘤生长.

体内活性: BQU57抑制H2122和H358细胞系中RalA与RalB活化,从而引起细胞生长抑制。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 16 mg/mL (47.9 mM)
DMSO : 61 mg/mL (182.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | BQU 57 | Ras | BQU57 | Inhibitor | BQU-57

相关产品: Tyrphostin 8 | Exo-1 | RBC8 | Compound C108 | CID-4785700 | Dynamin inhibitory peptide Acetate | RBC10 | CCG-63808 | CCG 203769 | CCG-50014

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Ferroptosis Compound Library | Fluorochemical Library | Inhibitor Library | Kinase Inhibitor Library | GPCR Compound Library | Autophagy Compound Library | Reprogramming Compound Library | Bioactive Compound Library

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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