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网站主页 化工产品目录 生物化工 抑制剂 细胞周期(Cell Cycle) CDK 抑制剂 SU 9516 化合物 SU9516
  • 化合物 SU9516|T6167|TargetMol

化合物 SU9516|T6167|TargetMol

SU9516
377090-84-1
￥263 1mg 起订
￥369 2mg 起订
￥578 5mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 SU9516
英文名称：
SU9516
CAS号：
377090-84-1
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：
99.94%
产品类别：
抑制剂
货号：
T6167

Product Introduction

Bioactivity

名称SU9516
描述SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
细胞实验Method: Cells are seeded at 2×103/well of white bottom 96-well plates, treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37 ℃ in an atmosphere containing 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.
激酶实验CDK kinase assay: Kinase assays are performed in 96-well polypropylene plates. Each reaction contained 2 μg of histone H1 at a final concentration of 10 μM [γ-33P]ATP (0.2 μCi/well; approximately twice the experimentally determined Km), 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol in a 40 μL volume. The reaction is initiated with the addition of 20 μL enzyme (6 ng cdk2/well resulting in a final concentration of 1.6 nM), which is previously diluted 1:50–1:200 in the same buffer, and allowed to proceed for 1 h at room temperature. Reaction is stopped by the addition of 0.01 mL 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is washed three times with 1.0% phosphoric acid, air dried, and then counted for radioactivity in a liquid scintillation counter. The cdk4 kinase assay for cyclin D1-cdk4 is carried out in a polypropylene 96-well microtiter plate format measuring the incorporation of radioactive phosphate into GST-Rb. Purified cyclin D1-cdk4 is incubated with 1 μg GST-Rb in 20 mM HEPES (pH 7.5) in the presence of 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol. The final cdk4 concentration is 10 ng/well, or 1.6 nM. Kinase reaction is initiated by the addition of ATP at a final concentration of 10 μM ATP (twice the experimentally determined Km) and [γ-33P]ATP (1.0 μCi per well) in a 60-μL volume and allowed to proceed at room temperature for 1 h. Reaction is stopped by the addition of 0.01 ml 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is treated as for Cdk1/Cdk2 assays.
体外活性SU9516降低了视网膜母细胞瘤蛋白pRB的cdk2特异性磷酸化作用，增加了caspase-3的活化，并改变了RKO和SW480细胞的细胞周期。此外，SU9516还抑制了这两种细胞系的细胞增殖，并诱导了细胞凋亡。[1] SU9516通过抑制RNA Pol II CTD的磷酸化、氧化损伤以及Mcl-1的转录下调，杀死了白血病细胞。[2] 在人T细胞白血病Jurkat细胞中，SU9516显著提高了对甲氨蝶呤的敏感性。[3] 此外，SU9516还抑制了Aurora-A的着丝粒定位和随之发生的着丝粒增倍。[4]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 55 mg/mL (227.98 mM)
Ethanol : 4.8 mg/mL (20 mM)
关键字Apoptosis | Autophagy | inhibit | CDK | Cyclin dependent kinase | SU9516 | SU-9516 | Inhibitor | SU 9516
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相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 成骨分子库 | 激酶抑制剂库 | 抗衰老化合物库 | 细胞骨架化合物库 | TGF-β/Smad靶点化合物库 | 疼痛相关化合物库
SU9516|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

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