- GSK 650394
| EMD638683SGK1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.46%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
| Description | EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 μM. | |||||
| Targets | SGK1 | |||||
| IC50 | 3 μM | |||||
| Cell experiment: [1] | |
Cell lines | HeLa-cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 10 μM , 24 hours |
Applications | As an inhibitor of SGK1, EMD638683 inhibited the phosphorylation of NDRG1 (N-Myc downstream-regulated gene 1), a specific target of SGK1. The IC50 value is 3.35 μM. |
| Animal experiment : [1] | |
Animal models | SGK1 deficient mice ((sgk1-/-) |
Dosage form | In chow, 600mg/kg, 4 days |
Applications | The tap drinking water was replaced by 10 % fructose for 3 weeks to develop hyperinsulinemia. Treatment of EMD638683 for four days led to normalization of systolic blood pressure (from 111 ± 4 to 87 ± 3 mmHg). It did not significantly modify fluid and food intake and did not significantly alter the urinary Na+ and K+ excretion, but significantly increased the urinary output and significantly decreased body weight. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Ackermann T F, Boini K M, Beier N, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cellular Physiology and Biochemistry, 2011, 28(1): 137-146. | |
EMD638683 Dilution Calculator
calculate
EMD638683 Molarity Calculator
calculate
| Cas No. | 1181770-72-8 | SDF | Download SDF |
| Synonyms | EMD 638683;EMD-638683 | ||
| Chemical Name | N"-[2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide | ||
| Canonical SMILES | CCC1=C(C=CC(=C1C)O)C(=O)NNC(=O)C(C2=CC(=CC(=C2)F)F)O | ||
| Formula | C18H18F2N2O4 | M.Wt | 364.34 |
| Solubility | ≥18.2 mg/mL in DMSO, ≥45.8 mg/mL in EtOH with gentle warming, <2.66 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
EMD638683 is a highly selective inhibitor of the serum and glucocorticoid inducible kinase (SGK) with IC50 value of 3 μM [1].SGK is a group of serine/threonine kinases that consists of SGK1, SGK2 and SGK3. Among these, SGK1 takes participate in the signaling pathway that regulates the sodium channel, cell proliferation, cell survival and many other cellular processes. The transcription of SGK1 can be up-regulated by the activation of serum, mineralocorticoids and glucocorticoids. SGK1 enhanced the renal tubular reabsorption of sodium after the high salt activation. Besides that, SGK is highly expressed in some sorts of tumors while down-regulated in some other tumors such as APC. The selective SGK1 inhibitor EMD638683 showed inhibition effects on all the three forms of SGK but not for other kinases. It can affect the phosphorylation of NDRG1in vitro and meanwhile exert anti-tumor or anti-hypertensive efficacy in vivo [1, 2].In the biochemical kinase assays, EMD638683 at concentration of 1 μM inhibited 85%, 71% and 75% activities of SGK1, SGK2 and SGK3, respectively. It also had inhibitory effects on MSK1 (mitogen-and stress-activated protein kinase 1) and PRK2 (protein kinase C-related kinase 2) with IC50 values of ≤ 1 μM. For other 64 kinases, such as MAPK, PRAK and Syk, EMD638683 showed no significant inhibition. In HeLa cells, EMD638683 suppressed the phosphorylation of NDRG1, which is a target of SGK1, with IC50 value of 3.35 μM. Besides that, EMD638683 treated CaCo-2 cells displayed increased depolarized mitochondria and enhanced caspase activity after the exposure to radiation [1, 2].In mice treated with the carcinogenic drugs, the administration of EMD638683 at dose of 600 mg/kg/day significantly lowered the colon weight and reduced the developing tumors. In another mice experiment, administration of EMD638683 increased the urinary output and normalized the systolic blood pressure in mice treated with 10% fructose drinking water. It indicated that EMD638683 might be an attracted drug for the hypertension treatment in diabetic patients [1, 2].References: [1] Towhid S T, Liu G L, Ackermann T F, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cellular physiology and biochemistry: international journal of experimental cellular physiology, biochemistry, and pharmacology, 2012, 32(4): 838-848.[2] Ackermann T F, Boini K M, Beier N, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cellular Physiology and Biochemistry, 2011, 28(1): 137-146.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
现在不少文献和讲座都提到使用化学成份限定的supplement代替蛋白水解物，大家有什么经验可以分享或者交流的吗？
1、血清：大部分人提及的Hyclone和Gibco，现在很多人对其血清的来源及目前市面上流行的真假好坏有怀疑，有人买到说好，有人说像是假的；也有人用国产的胎牛血清培养的，多提及兰州民海和四季青的，并且对兰州民海似乎支持者较多。对血清的选择还想说，不同厂家不同批次的血清都不同保证成分完全一致，对于使用者而言，可以从外观、培养方面了解血清的质量。
2、内皮生长因子：养内皮细胞都需加入生长因子，ECGS和ECGF用的较多，含量ECGS0.03-0.05mg/ml或ECGF50μg/ml，品牌提的最多的是Sigma的，但是Sigma的真心贵啊，另有些人提的最多的是罗氏，较便宜，75mg才2200RMB左右，性价比应该是比较高的，本人准备入手。
3、肝素：肝素在内皮细胞培养中的作用是抑制其他杂细胞的生长，尤其是平滑肌细胞的生长，使内皮细胞成为生长优势群，浓度不定，有几种说法：查阅书，15μg/ml；美国ATCC说明书，0.1mg/ml；另有50U/ml，肝素买的话大部分人也都推荐Sigma。
2014年10月21日08:55:05来源：中国青年报
“在我国，90%左右的人认为食品安全问题是食品添加剂所造成的，但很多人把非法添加物误认为是食品添加剂。”在近日召开的中国食品安全年会上，中国工程院院士孙宝国解释了食品添加剂与非法添加物的不同。
他指出，食品添加剂的使用有着6点需要，首先是为了改善食品品质。以婴幼儿配方奶粉为例,许多婴幼儿奶粉中正是因为添加了符合标准的食品添加剂，才能最大程度地接近母乳成分。
其次，使用食品添加剂是食品防腐的客观需要。“很多消费者对防腐剂表示反感，但如果食品中没有防腐剂，那么有害的微生物就会迅速繁殖，而有害微生物污染恰恰是造成食品安全问题的第一大杀手。”孙宝国强调。
除此之外，他还指出，食品添加剂可以起到让食品保鲜、改善食品色香味、满足食品加工工艺等需求。“可乐里面一定含有咖啡因，因为没有咖啡因成分的话，就不可能称之为可乐。”孙宝国表示，从毒理学角度看，不少食品添加剂的确有毒，如卤水，但食品添加剂本身有毒与添加了食品添加剂的食品有毒绝对是两回事，主要区别在于食品添加剂的使用量。
“食品添加剂只要合法使用都是安全的，不会对人体健康造成危害，因此，一定要监管好食品添加剂的使用，违法使用，超量、超范围使用都有可能带来风险”。孙宝国说。
国家食品安全风险评估中心首席科学家吴永宁也指出，当前食品安全控制的应该是风险，而不是危害。“我们要规范好什么样的食品添加剂能用，以及使用剂量和使用范围。如果在规范之外，就是非法添加。三聚氰胺、苏丹红这些都是非法添加物，我们不能把非法添加物与食品添加剂进行混淆。”
相容性药品包装材料与药物相容性试验指导原则2.pdf(43.35k)
