化合物GSK923295 T2039
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 |
---|---|---|---|
2 mg | 1088965-37-0 | ¥626.00 | 询底价 |
25 mg | 1088965-37-0 | ¥3,190.00 | 询底价 |
1 mg | 1088965-37-0 | ¥433.00 | 询底价 |
1 mL | 1088965-37-0 | ¥1,290.00 | 询底价 |
100 mg | 1088965-37-0 | ¥6,760.00 | 询底价 |
5 mg | 1088965-37-0 | ¥917.00 | 询底价 |
10 mg | 1088965-37-0 | ¥1,550.00 | 询底价 |
50 mg | 1088965-37-0 | ¥4,730.00 | 询底价 |
Product Introduction
Bioactivity
英文名: GSK-923295
描述: GSK923295 是一种特异性的变构着丝粒相关蛋白-E 驱动蛋白 ATPase 活性抑制剂,作用于人类和犬类此酶,Ki 分别为 3.2±0.2 nM 和 1.6±0.1 nM。
细胞实验: Cell-growth inhibition assays are performed by MDS in 384-well plates, and DNA content of fixed cells stained with DAPI using an Incell 1000 is analyzed. DNA content is determined 24 h after seeding (T0) and after exposure to varying concentrations of drug for an additional 72 h (T72). All T72 measurements are normalized to T0. Curves are analyzed using the XLfit curve-fitting tool to determine the concentration of GSK923295 yielding 50% growth inhibition relative to T0 and Ymax values (GI50).(Only for Reference)
激酶实验: Enzymology: Kinesin motor domains are expressed in Escherichia coli BL21(DE3) and purified. CENP-E proteins includes residues 2–340 with a carboxyl-terminal 6-his tag. All studies using MT are conducted in PEM25 buffer [25 mM PipesK+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM MT, and 1 nM CENP-E in PEM25 buffer.
体外活性: 在多种实体瘤模型中,如尤因肉瘤,杆状瘤,横纹肌肉瘤移植瘤,GSK923295均能产生显著地抗肿瘤活性.Colo205移植瘤中,GSK923295(125 mg/kg)能够抑制肿瘤生长,使核分裂和游离的凋亡小体明显增加.
体内活性: 在癌细胞系中,GSK923295具有广谱抗肿瘤活性,对于 SW48(IC50=17.2 nM), RKO (BRAF mutant)( IC50=55.6 nM), SW620 (KRAS mutant)(IC50=42 nM), and HCT116 (KRAS mutant)(IC50=51.9 nM)。在人类神经母细胞瘤细胞系中,GSK923295平均生长IC50为41 nM。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 93 mg/mL (157.1 mM)
DMSO : 93 mg/mL (157.1 mM)
关键字: GSK923295 | inhibit | Inhibitor | Apoptosis | GSK 923295 | Kinesin | GSK-923295
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相关库: Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | NO PAINS Compound Library
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