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  • 化合物 COH29|T3157|TargetMol

化合物 COH29|T3157|TargetMol

COH29
1190932-38-7
￥768 1mg 起订
￥1130 2mg 起订
￥1890 5mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

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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 COH29
英文名称：
COH29
CAS号：
1190932-38-7
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：
98.92%
产品类别：
抑制剂
货号：
T3157

Product Introduction

Bioactivity

名称COH29
描述COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis.
细胞实验Cells is seeded into 96-well plates in 100 μL of complete medium at 2000 to 5000 cells per well, depending on the cell line's growth rate. After overnight incubation, test compound is added to each well at various concentrations in 50 μL of culture medium. After a further incubation for 96 hours at 37°C, fluorescein diacetate (final concentration: 10 mg/mL) and eosin Y [final concentration: 0.1% (w/v)] is added to each well, and the cells is incubated for an additional 20 minutes at 37°C. Cytotoxicity is assessed by Digital Imaging Microscopy System detection Viability is assessed using MTS [(3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium)] as previously described[1].
激酶实验For kinase assays following immunoprecipitation of FLAG-CDK7 protein from HCT116 or FLAG-CDK12 from 293A cellular lysates, cells are first treated with THZ1, THZ1-R, or DMSO for 4 hrs at 37°C. Cells are then harvested by lysis in 50 mM Tris HCl pH 8.0, 150 mM NaCl, 1% NP-40, 5 mM EDTA, and protease/phosphatase cocktails. Exogenous CDK7 or CDK12 proteins are immunoprecipitated from cellular lysates using FLAG antibody- conjugated agarose beads. Precipitated proteins are washed with lysis buffer 6 times, followed by 2 washes with kinase buffer (40 mM Hepes pH 7.5, 150 mM NaCl, 10 mM MgCl2, 5% glycerol) and subjected to in vitro kinase assays at 30°C for 45 minutes using 1 μg of the large subunit of RNAPII (RPB1) as substrate and 25 μM ATP and 10 μCi of 32P ATP. Kinase assays using recombinant CDK7/TFIIH/MAT1 are conducted in the manner as described above using 25 ng of CAK complex per reaction. For kinase assays designed to test time-dependent inactivation of CDK7 kinase activity, CAK complex is pre-incubated with indicated concentrations of THZ1, THZ1-R, or DMSO in kinase buffer without ATP for 4 hrs at 30°C prior to being subjected to kinase assay conditions[1].
体外活性COH29成功克服了Y细胞对吉西他滨和羟基脲的抗药性。在NCI 60人类Y系列的大多数细胞系中，它强效抑制增殖，但对正常成纤维细胞或内皮细胞几乎无影响。NMR、定点突变技术和表面等离子体共振生物传感器研究确认COH29与提议的配体结合口袋结合，并为RRM1-RRM2四聚体结构的组装阻断提供了证据[1]。
体内活性COH29 (50/100 mg/kg, b.i.d., p.o.)在MOLT-4肿瘤移植模型中显示出剂量依赖性的抑制增长效果，尤其在治疗第12天时抑制效果显著。在携带TOV11D肿瘤移植物的小鼠中，连续7天使用COH29 (200/300/400 mg/kg/天)同样展示出剂量依赖性的肿瘤生长抑制效果。与对照组相比，肿瘤增长被显著抑制[1]。
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 : 50 mg/mL (118.92 mM)
关键字subunit | RNR Inhibitor COH-29 | RNR Inhibitor COH 29 | RNR | ribonucleotide | reductase | Inhibitor | inhibit | DNA/RNA Synthesis | COH-29 | COH29 | COH 29 | anticancer
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相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌化合物库 | 已知活性化合物库 | 细胞周期化合物库 | 细胞凋亡化合物库 | 抗衰老化合物库 | 临床期小分子药物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
RNR Inhibitor COH29|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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