SR-12813

Modify Date: 2024-01-02 18:08:24

SR-12813 Structure
SR-12813 structure
Common Name SR-12813
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-12813


SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.

 Names

Name sr12813
Synonym More Synonyms

 SR-12813 Biological Activity

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

[1]. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.

[2]. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.

 Chemical & Physical Properties

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℃

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport

 Articles4

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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.

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 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
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