- GSK 650394
EMD638683SGK1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.46%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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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. |
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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="">2.66> | 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.
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grace粉末来配制,按说明书上的话加入碳酸氢钠外就不用加入
别的东西了,请问是否可以直接过滤用了:
在问,我们同一楼的另外一个实验室配制的时候加入了
水解乳蛋白和酵母粉,是否有这个必要,谢谢.在线,急等
不过因为食品添加剂种类很多,适应范畴和添加量都是规定的,如果你未按gb2760的规定使用,可能构成违法,具体是否是犯罪,要看具体的性质。
比如:二氧化钛(就是食品级的钛白粉)允许在允许在膨化食品、果冷、凉果等类限量使用,如果你在肉制品中使用,属于超范围墙使用,就是违法行为。
其次是超量使用,一般超量使用,又没有构成严重后果,属滥用食品添加剂,一般不按犯罪处理。
但超范围使用,加上媒体炒作的话,可能就麻烦了,因为公-安-执-法部门对此不太专业,往往会有意无意的扩大化,有可能会按刑法143条,生产销售伪劣食品罪起诉。
要注意:食品添加剂和非法添加物的区别,食品添加剂是国家允许使用的物质,而非法添加剂则是指食品及添加剂以外的物质,如三聚氰胺、吊白块、苏丹红等,不是食品添加剂,如果使用此类物质,则构成犯罪。
求助日本《医药品添加物事典》关于羟苯丙酯钠在口服溶液剂中最大用量
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)
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