Hymeglusin (Synonyms: Antibiotic 1233A) |
| Catalog No.GC43883 |
Hymeglusin is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 29066-42-0
Sample solution is provided at 25 µL, 10mM.
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Hymeglusin is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.[1][2] At a dose of 25 mg/kg, hymeglusin inhibits cholesterol biosynthesis in rats by 45%. Chiral studies indicate that the (2R,3R)-β-lactone moiety of hymeglusin is important for eliciting the specific inhibition of HMG-CoA synthase.[3] As a cell-wall targeting antibiotic, hymeglusin has been used to investigate the role of a gene important for controlling S. aureus virulence in a mouse sepsis model of infection.[4]
Reference:
[1]. Greenspan, M.D., Yudkovitz, J.B., Lo, C.Y., et al. Inhibition of hydroxymethylglutaryl-coenzyme A synthase by L-659,699. Proc. Natl. Acad. Sci. U.S.A. 84(21), 7488-7492 (1987).
[2]. Tomoda, H., Ohbayashi, N., Morikawa, Y., et al. Binding site for fungal β-lactone hymeglusin on cytosolic 3- hydroxy-3-methylglutaryl coenzyme A synthase. Biochim. Biophys. Acta 1636(1), 22-28 (2004).
[3]. Tomoda, H., Ohbayashi, N., Kumagai, H., et al. Differential inhibition of HMG-CoA synthase and pancreatic lipase by the specific chiral isomers of β-lactone DU-6622. Biochem. Bioph. Res. Commun. 265(2), 536-540 (1999).
[4]. Balibar, C.J., Shen, X., McGuire, D., et al. cwrA, a gene that specifically responds to cell wall damage in Staphylococcus aureus. Microbiology 156(Pt 5), 1372-1383 (2010).
| Cas No. | 29066-42-0 | SDF | |
| Synonyms | Antibiotic 1233A | ||
| Chemical Name | 11-[3R-(hydroxymethyl)-4-oxo-2R-oxetanyl]-3,5,7R-trimethyl-2E,4E-undecadienoic acid | ||
| Canonical SMILES | OC[C@@H](C1=O)[C@H](O1)CCCC[C@@H](C)C/C(C)=C/C(C)=C/C(O)=O | ||
| Formula | C18H28O5 | M.Wt | 324.4 |
| Solubility | Soluble in ethanol, or in methanol, or in DMSO, or in chloroform | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0826 mL | 15.4131 mL | 30.8261 mL |
| 5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0826 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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