Application | Comment | Organism |
---|---|---|
medicine | small-molecule S1P inhibitors are capable of reducing cholesterol and fatty acid synthesis in vivo and, therefore, represent a potential new class of therapeutic agents for dyslipidemia and for a variety of cardiometabolic risk factors associated with diabetes, obesity, and the metabolic syndrome | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
cDNA encoding amino acids 17 to 997, encompassing the prodomain, catalytic domain, and cysteine-rich domain of soluble site 1 protease (sS1P) is expressed in CHO cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide | inhibits endogenous SREBP processing in Chinese hamster ovary cells. Compound down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In mice treated with the compound for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced | Homo sapiens | |
(S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide | purified S-enantiomer | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q14703 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Ac-VFRSLK-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | ? | - |
? | |
Dabcyl-Arg-His-Ser-Ser-Arg-Arg-Leu-Leu-Arg-Ala-Leu-Glu-Gly-Gly-Lys(tetramethylrhodamine)-OH + H2O | - |
Homo sapiens | ? | - |
? | |
Dabcyl-Ser-Gly-Ser-Gly-Arg-Ser-Val-Leu-Ser-Phe-Glu-Ser-Gly-Ser-Lys(tetramethylrhodamine)-Arg-OH + H2O | - |
Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
S1P | - |
Homo sapiens |
SREBP site 1 protease | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000175 | - |
inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells | Homo sapiens | (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide | |
0.000393 | - |
inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells | Homo sapiens | (S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide | |
0.0005 | - |
in HepG2 cells, compound inhibits cholesterol synthesis, with an IC50 of 0.0005 mM | Homo sapiens | (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide | |
0.000971 | - |
purified S-enantiomer, inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells | Homo sapiens | (S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide |