SR-12813
SR-12813 structure
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Common Name | SR-12813 | ||
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| CAS Number | 126411-39-0 | Molecular Weight | 504.53400 | |
| Density | 1.117g/cm3 | Boiling Point | 552.6ºC at 760mmHg | |
| Molecular Formula | C24H42O7P2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | 288ºC | |
Use of SR-12813SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. |
| Name | sr12813 |
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| Synonym | More Synonyms |
| Description | SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. |
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| Related Catalog | |
| Target |
IC50: 0.85 μM (HMG-CoA Reductase) |
| In Vitro | SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM[1]. Both 25-HC and SR-12813 can kill mammalian cells through blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection. SR-12813 kills HeLa cells at concentration range from 8 µM to 16 µM. SR-12813 kills wild type cells and mutant cells infected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotes the degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and SL-5 mutant cells[1]. |
| Kinase Assay | Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure “total” HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined. |
| References |
| Density | 1.117g/cm3 |
|---|---|
| Boiling Point | 552.6ºC at 760mmHg |
| Molecular Formula | C24H42O7P2 |
| Molecular Weight | 504.53400 |
| Flash Point | 288ºC |
| Exact Mass | 504.24100 |
| PSA | 110.91000 |
| LogP | 7.81780 |
| Vapour Pressure | 8.02E-13mmHg at 25°C |
| Index of Refraction | 1.504 |
| Storage condition | -20℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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Dehydroepiandrosterone induces human CYP2B6 through the constitutive androstane receptor.
Drug Metab. Dispos. 35 , 1495-501, (2007) Dehydroepiandrosterone (DHEA), the major precursor of androgens and estrogens, has several beneficial effects on the immune system, on memory function, and in modulating the effects of diabetes, obesi... |
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Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells.
J. Biol. Chem. 283 , 30650-7, (2008) The human pregnane X receptor (hPXR) regulates the expression of critical drug metabolism enzymes. One of such enzymes, cytochrome P450 3A4 (CYP3A4), plays critical roles in drug metabolism in hepatoc... |
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Isolation of mutant cells lacking Insig-1 through selection with SR-12813, an agent that stimulates degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.
J. Biol. Chem. 279 , 43136-47, (2004) Insig-1 and Insig-2 are membrane proteins of the endoplasmic reticulum that regulate lipid metabolism by the following two actions: 1) sterol-induced binding to 3-hydroxy-3-methylglutaryl-coenzyme A r... |
| Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate |
| SRL |
| HTMT dimaleate |
| 1ilh |
| 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol |
| BIDD:PXR0009 |
| SR 12813 |