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EN40 Sale

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。

EN40 Chemical Structure

Cas No.:2094547-67-6

规格 价格 库存
5mg
¥4,050.00
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10mg
¥6,750.00
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25mg
¥12,150.00
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50mg
¥20,250.00
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100mg
¥30,150.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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

Chemical Properties

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.
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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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溶解性数据

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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
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Research Update

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.