| CAS: | 13616-29-0 | |
| 分子式: | C23H22N8O5S2 | |
| 分子量: | 554.60 | |
| 中文名称: |
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| 英文名称: |
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| 用途: | GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors. |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||||||||||||||||
| N920957 | MACKLIN | N，N'-二[4-（4-甲基-嘧啶-2-基氨磺酰基）苯基]-脲 | ≥98% (HPLC) | 1332元/5mg; | 咨询 | ||||||||||||||||||||||||||||||||||||||||||
储存：2-8°C 状态：固体 | |||||||||||||||||||||||||||||||||||||||||||||||
| G5547 | Sigma-Aldrich | GSK837149A | ≥98% (HPLC), solid | 1480.38元/5 MG; | 咨询 | ||||||||||||||||||||||||||||||||||||||||||
产品说明 包装 5, 25 mg in glass bottle 生化/生理作用 GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors. 特点和优势 This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here. 基本信息
产品性质
安全信息
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| HY-117769 | MCE | GSK837149A,13616-29-0_MCE(MedChemExpress) | 666元/1 mg; 1980元/5 mg; | 咨询 | |||||||||||||||||||||||||||||||||||||||||||
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。 GSK837149AMCE 国际站：GSK837149A 品牌：MedChemExpress (MCE) 货号：HY-117769 CAS 号：13616-29-0 生物活性： GSK837149A 是一种选择性抑制人脂肪酸合成酶 (FASN) 的抑制剂，靶向 KR 结构域。GSK837149A 对 FASN 具有可逆性抑制作用，且对 I 型 FASN 具有选择性 (Ki=30 nM)。GSK837149A 也是 NADPH 的竞争性抑制剂和乙酰乙酰辅酶 A 的非竞争性抑制剂。GSK837149A 可用于肥胖症和乳腺癌的研究[1][2]。 体外研究(In Vitro)：GSK837149A (0.1 nM-0.1 mM) 对乙酰辅酶 A/丙二酰辅酶 A 和乙酰乙酰辅酶 A 的抑制作用随作用浓度增加而增强[1]。 MCE尚未独立确认这些方法的准确性。 仅供参考。 分子量：554.60 Formula：C23H22N8O5S2 性状：固体 颜色：White to off-white 运输条件：美国大陆地区的室温；其他地区可能有所不同。 储存方式：粉末 -20°C 3年 提供质量检测报告：Data Sheet、SDS、COA、LCMS、元素分析报告、产品使用指南 产品活性：GSK837149A 是人脂肪酸合成酶 (FASN) 的选择性抑制剂，靶向 KR 结构域。GSK837149A 对 FASN 具有可逆抑制作用，对 I 型 FASN (Ki=30 nM) 具有选择性。GSK837149A 也是 NADPH 的竞争性抑制剂和乙酰-乙酰-辅酶 A 的非竞争性抑制剂。GSK837149A 可用于肥胖和乳腺癌的研究。 IC50 & Target：Ki: 30 nM (type I FASN)[1] 相关产品：Mulberroside F | Coenzyme A | Denifanstat | Malic enzyme inhibitor ME1 | PF429242 dihydrochloride | C75 | Coenzyme A sodium | TVB-3664 | Coenzyme A trilithium | CY5-SE | CY5-SE (solution) | FASN-IN-4 tosylate 热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类 Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides MCE 抑制剂: MedChemExpress 信号通路产品覆盖细胞凋亡、自噬、细胞周期与 DNA 损伤、表观遗传、GPCR/G 蛋白、免疫与炎症、JAK/STAT、MAPK/ERK、膜转运体与离子通道、代谢酶与蛋白酶、神经信号、NF-κB、PI3K/Akt/mTOR、PROTAC、蛋白酪氨酸激酶/受体酪氨酸激酶、干细胞/Wnt、TGF-β/Smad 及维生素 D/核受体等研究方向，为肿瘤、感染、炎症与免疫、神经系统疾病、代谢性疾病、心血管疾病和内分泌研究提供多维度的产品选择，助力客户发表文献超 80,000 篇。 相关产品可根据具体情况提供化学结构、作用靶点、生物活性、纯度、溶解度、体内外研究信息、参考文献及质量分析报告 (COA)等资料。 客户发表文献： 参考文献： 品牌介绍:
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