126411-39-0
126411-39-0 structure
- Name: SR-12813
- Chemical Name: sr12813
- CAS Number: 126411-39-0
- Molecular Formula: C24H42O7P2
- Molecular Weight: 504.53400
- Catalog: Signaling Pathways Metabolic Enzyme/Protease HMG-CoA Reductase (HMGCR)
- Create Date: 2017-07-18 13:12:05
- Modify Date: 2024-01-02 18:08:24
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SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.
| Name | sr12813 |
|---|---|
| Synonyms |
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 |
| Description | SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM. |
|---|---|
| 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 |
|---|---|
| RIDADR | NONH for all modes of transport |