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网站主页 化工产品目录 生物化工 抑制剂 细胞骨架(Cytoskeletal Signaling) Kinesin 抑制剂 SB 743921; (R)-N-(3-AMINOPROPYL)-N-(1-(3-BENZYL-7-CHLORO-4-OXO-4H-CHROMEN-2-YL)-2-METHYLPROPYL)-4-METHYLBENZAMIDE HYDROCHLORIDE 化合物 SB743921
  • 化合物 SB743921|T2255|TargetMol

化合物 SB743921|T2255|TargetMol

SB-743921 hydrochloride
940929-33-9
623 2mg 起订
947 5mg 起订
1680 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 SB743921
英文名称:
SB-743921 hydrochloride
CAS号:
940929-33-9
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
≥95%
产品类别:
抑制剂
货号:
T2255

Product Introduction

Bioactivity

NameSB-743921 hydrochloride
DescriptionSB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).
Cell ResearchAll cells including HeLa cells are cultured in 10% FCS in RPMI 1640 in 5% CO2. We assessed 48-hour growth inhibition by serial dilution of SB 743921 relative to DMSO-treated cells in 96-well microtiter plates, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium. Cell growth is represented as the ratio of absorbance of treated cells to DMSO control, plotted by concentration and fitted to a four-parameter curve. Concentrations at which cellular growth is inhibited by 50% are extrapolated from the curve fit. The DNA content of HeLa cells cultured in the presence or absence of 1 μM SB 743921 for 24 hours is assessed by propidium iodide staining and flow cytometry. Immunofluorescence images are collected of HeLa cells treated for 24 hours with 1 μM SB 743921, fixed with 2% formaldehyde, permeabilized, and stained with DM1-α, anti-γ-tubulin, and 1 μg/mL 4′,6-diamidino-2-phenylindole, and with Alexa 488 secondary goat antirabbit IgG and Rhodamine-X goat antimouse IgG. Images are collected with a DeltaVision Restoration Microscopy System at a magnification of ×600. Z stacks (0.2 μm) are collected, and out of focus information is removed by constrained iterative deconvolution. Z stacks are then compressed into to a single image plane. (Only for Reference)
Kinase AssayBiochemistry assay: The motor domains of KSP (amino acids 1–360) is expressed as in Escherichia coli BL21(DE3) as COOH-terminal 6-his fusion proteins. Bacterial pellets are lysed in a microfluidizer with a lysis buffer [50 mM Tris-HCl; 50 mM KCl, 10 mM imidazole, 2 mM MgCl2, 8 mM β-mercaptoethanol, 0.1 mM ATP (pH 7.4)], and proteins are purified using Ni-NTA agarose affinity chromatography, with an elution buffer consisting of 50 mM PIPES, 10% sucrose, 300 mM imidazole, 50 mM KCl, 2 mM MgCl2, mM β-mercaptoethanol, and 0.1 mM ATP (pH 6.8). Steady-state measurements of ATPase activity are performed with a pyruvate kinase–lactate dehydrogenase detection system that coupled the appearance of ADP with oxidation of NADH. Absorbance changes are monitored at 340 nm. All biochemical experiments are performed in PEM25 buffer [25 mM Pipes/KOH (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM SB 743921 for experiments involving microtubules. Rates of ADP release are measured in a stopped-flow apparatus; the decrease in fluorescence of MANT-ATP is monitored. Rates of Pi release are measured in a stopped-flow apparatus, using bacterial phosphate binding protein modified with 7-diethylamino-3-((((2 maleimidyl)ethyl)amino)carbonyl)coumarin (MDCC) dye. Ki estimates of KSP inhibitors are extracted from the dose–response curves, with explicit correction for enzyme concentration. Tubulin polymerization by measuring changes in absorbance at 340 nm is monitored. The assay is performed in 100-μL volumes in 96-well half-area microtiter plates, using a microplate reader with the incubation temperature set at 37 °C.
In vitro对于多种异种移植人的肿瘤,如Colo205,MCF-7, SK-MES, H69, OVCAR-3HT-29, MX-1, MDA-MB-231, A2780,SB-743921均能产生明显的抑制效应,抑制细胞生长的活性.
In vivoSB 743921阻断了有丝分裂纺锤体的产生,因此能将细胞在有丝分裂期积累并产生细胞坏死,对于人的KSP(Ki=0.1 nM)和鼠的KSP(Ki=0.12 nM)。
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 60 mg/mL (108.4 mM), Sonication is recommended.
KeywordsSB743921 Hydrochloride | Kinesin | SB743921 hydrochloride | SB 743921 Hydrochloride | inhibit | SB-743921 Hydrochloride | SB 743921 hydrochloride | Inhibitor | SB-743921 | SB 743921
Inhibitors RelatedS-trityl-L-Cysteine | Paprotrain | Monastrol | Eg5-IN-1 | Empesertib | UMK57 | BRD9876 | CW-069 | Eg5 Inhibitor V, trans-24 | BAY1217389 | AZD-4877 | MPI-0479605
Related Compound LibrariesInhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | ReFRAME Related Library | Highly Selective Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library
SB743921 HCl|||SB743921|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 SB743921相关厂家报价

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