EN40
目录号 : GC38909
EN40 是一种有效的选择性乙醛脱氢酶 3A1 (ALDH3A1) 抑制剂，一种共价配体，IC50 值为 2 uM。
Cas No.:2094547-67-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM[1]
EN40 (10-1000 μM; 48 hours) shows inhibitory effecton ALDH3A1 activity and impairs A549 cell survival[1]. Cell Viability Assay[1] Cell Line: A549 cells
EN40 (intraperitoneal injection; 50mg/kg; from 14 days; once per day) exerts strong anti-tumorigenic effects in established A549 tumor xenografts, shows good tolerability with no body weight loss in mice[1]. Animal Model: SCID mice with A549 cells[1]
[1]. Counihan JL,et al.Chemoproteomics-Enabled Covalent Ligand Screening Reveals ALDH3A1 as a Lung Cancer Therapy Target.ACS Chem Biol. 2018 Aug 17;13(8):1970-1977
| Cas No. | 2094547-67-6 | SDF | |
| Canonical SMILES | C=CC(N1CCC(C)=C(C2=CC=CO2)C1)=O | ||
| 分子式 | C13H15NO2 | 分子量 | 217.26 |
| 溶解度 | DMSO: 5 mg/mL (23.01 mM); Ethanol: 2 mg/mL (9.21 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6028 mL | 23.0139 mL | 46.0278 mL |
| 5 mM | 0.9206 mL | 4.6028 mL | 9.2056 mL |
| 10 mM | 0.4603 mL | 2.3014 mL | 4.6028 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Chemoproteomics-Enabled Covalent Ligand Screening Reveals ALDH3A1 as a Lung Cancer Therapy Target
ACS Chem Biol 2018 Aug 17;13(8):1970-1977.PMID:30004670DOI:10.1021/acschembio.8b00381.
Chemical genetics is a powerful approach for identifying therapeutically active small molecules, but identifying the mechanisms of action underlying hit compounds remains challenging. Chemoproteomic platforms have arisen to tackle this challenge and enable rapid mechanistic deconvolution of small-molecule screening hits. Here, we have screened a cysteine-reactive covalent ligand library to identify hit compounds that impair cell survival and proliferation in nonsmall cell lung carcinoma cells, but not in primary human bronchial epithelial cells. Through this screen, we identified a covalent ligand hit, DKM 3-42, which impaired both in situ and in vivo lung cancer pathogenicity. We used activity-based protein profiling to discover that the primary target of DKM 3-42 was the catalytic cysteine in aldehyde dehydrogenase 3A1 (ALDH3A1). We performed further chemoproteomics-enabled covalent ligand screening directly against ALDH3A1, and identified a more potent and selective lead covalent ligand, EN40, which inhibits ALDH3A1 activity and impairs lung cancer pathogenicity. We show here that ALDH3A1 represents a potentially novel therapeutic target for lung cancers that express ALDH3A1 and put forth two selective ALDH3A1 inhibitors. Overall, we show the utility of combining chemical genetics screening of covalent ligand libraries with chemoproteomic approaches to rapidly identify anticancer leads and targets.
A novel 62-bp indel mutation in the promoter region of transforming growth factor-beta 2 (TGFB2) gene is associated with body weight in chickens
Anim Genet 2011 Feb;42(1):108-12.PMID:20477792DOI:10.1111/j.1365-2052.2010.02060.x.
Transforming growth factor-beta 2 (encoded by TGFB2) is a growth factor that regulates a plethora of cellular functions. In this study, we sequenced the promoter and full-length exon region of the chicken TGFB2 and found two mutations (g.-640 C>T and g.-851 -790 del) within the promoter. The two polymorphisms were genotyped in 1030 pedigreed hens recorded for body weight at 7 (BW7), 9 (BW9), 11 (BW11), 13 (BW13), 17 (BW17) weeks old, egg weight at 36 weeks of age (EW36) and egg numbers from the age at first egg (AFE) to 40 weeks of age (EN40). Despite the fact that no mutations were found to have statistically significant genetic effects on egg production, the association results of growth traits showed that both g.-640 C>T and g.-851_-790del had significant effects on body weights and that both genotype g.-640 TT and g.-851_-790 wt/wt were positive for body weight performance. Therefore, the polymorphisms of TGFB2, especially the g.-851_-790del mutation associated with body weight at almost all periods, could be potential useful genetic markers to improve the growth of Beijing You chickens.