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网站主页 (1R,4S)-二甲基1-((R)-1-(苯基氨基)-2-(对甲苯基)乙基)-7-氧杂二环[2.2.1]庚-2,5-二烯-2,3-二羧酸 化合物 COH000
  • 化合物 COH000|T5199|TargetMol

化合物 COH000|T5199|TargetMol

COH000
1534358-79-6
￥1860 1mg 起订
￥2810 2mg 起订
￥4850 5mg 起订
上海 更新日期：2024-09-30

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 COH000
英文名称：
COH000
CAS号：
1534358-79-6
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：
99.23%
产品类别：
抑制剂
货号：
T5199

Product Introduction

Bioactivity

名称COH000
描述COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
细胞实验Cell proliferation was measured using a CellTiter 96 AQueous One Solution Cell Proliferation Assay (MTS-based) after COH000 or its analog (54 or 55) treatment at the indicated concentrations and the time points. Briefly, cells were incubated with 20 mL of CellTiter 96 AQueous reagentafter the treatment and incubated at 37C until color development. Absorbance measurements were performed using a SpectraMax M5 reader. For assays measuring anti-proliferation effects, all values were normalized to the vehicle treatment. All values are represented graphically as mean ± standard deviation (STDEV) from three independent samples (n=3).
激酶实验Briefly, SAE, Ubc9, GST-SUMO and His6-RanGap-1 proteins were expressed and purified as described previously.Assay buffer contained 50 mMTris-HCl pH 7.4, 0.3 mM DTT, 10 mM MgCl2, and 0.005% Tween-20. The assays were conducted using 1536-well, white plates. 2 μL of Mixture 1, containing 12.5 nM SAE and 100 nM His6-RanGap-1 in the assay buffer was mixed with 70 nl of 2 mM compounds dissolved in DMSO. Then 2 μL of Mixture 2, containing 20 mM ATP, 12.5 nM E2 and 30 nM GST-SUMO in assay buffer, was added. After incubation for 90 min at room temperature, 1 μl of pre-mixed Ni acceptor beads and Glutathione Donor beads, at 10 μg/ml each, was added. After incubation for 60 min at room temperature, readings were made on a BMG LabtechPheraStar in an AlphaScreen mode (Ex: 680 nm; Em: 570 nm).
动物实验Mice were housed in a controlled environment (12-h light/12-h dark cycle) with access to waterand fed a standard diet generally from 6 to 8 weeks of age. Body weight was measured weekly and food intake was monitored. For colorectal cancer xenograft with COH000 treatment, HCT116 cells were s.c. injected into a plasma esterase-deficient SCID mouse strain (Es1e/SCID), male, 8-10 weeks. When the tumors became palpable, COH000 was administered subcutaneously peritumoral injection once a day at a dose of 10 mg per kilogram of body weight. Mice in the control group received equal volumes of vehicle (5% DMSO, 30% solutol in PBS). Tumor volume was measured until the endpoint was reached. Mice were euthanized using CO2 inhalation and tumors were excised.
体外活性COH000在体外平均IC50约为0.2 μM的条件下抑制了SUMOylation，但在相同条件下，即使浓度高达100 μM，在以Ubc13介导的多聚泛素化试验中也未能抑制泛素化。COH000处理诱导了HCT-116细胞中的凋亡。通过转染过表达SAE2，凋亡水平降低；而当在HCT116细胞中敲除SAE2时，凋亡水平增加。
体内活性当肿瘤变得可触及时，携带肿瘤的Es1e/SCID小鼠接受了COH000或对照剂的治疗，为期14天。COH000显著抑制了肿瘤生长，并且显著降低了肿瘤组织中SAE2的水平。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 0.1 mg/mL (insoluble)
DMSO : 35.71 mg/mL (85.13 mM), Sonication is recommended.
关键字Ubiquitin conjugating enzyme | E1 activating enzyme | COH000 | E1/E2/E3 Enzyme | E2 conjugating enzyme | Ubiquitin ligase | Ubiquitin activating enzyme | COH-000 | COH 000 | Inhibitor | E3 ligating enzyme | inhibit
相关产品Nutlin-3 | NAE-IN-M22 | BC-1382 | RG7112 | NSC697923 | Indole-3-carbinol | PYR-41 | Idasanutlin | Navtemadlin | NAcM-OPT | PYZD-4409 | NSC232003
相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | HIF-1化合物库 | NO PAINS 化合物库 | 泛素化化合物库 | 表型筛选靶点鉴定库 | 共价抑制剂库
COH000|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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