Lactacystin (Synthetic) |
| Catalog No.: GC13123 |
Proteasome inhibitor
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
C6 cells |
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Preparation method |
The solubility of this compound in sterile water is 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
2.5, 5 or 10 μM |
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Applications |
Compared with no treatment, Lactacystin significantly inhibited the proliferation of C6 cells at the 3 indicated doses. In addition, Lactacystin at all concentrations also significantly increased the number of apoptotic cells and decreased mitochondrial membrane potential when compared with the control group. |
| Animal experiment [1]: | |
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Animal models |
Nude mice bearing gliomas |
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Dosage form |
1.0 μg or 5.0 μg per 20 g body weight; i.p.; q.d., for 7 days |
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Applications |
In nude mice bearing gliomas, Lactacystin significantly inhibited tumor growth. However, at day 17, tumor volume increased to baseline in all experimental groups. On day 9 after termination of Lactacystin treatment, the tumor staining results revealed that Lactacystin significantly increased the mRNA and protein levels in the ratio of Bax to Bcl-2. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Wang H, Zhang S, Zhong J, et al. The proteasome inhibitor lactacystin exerts its therapeutic effects on glioma via apoptosis: An in vitro and in vivo study. Journal of International Medical Research, 2013, 41(1): 72-81. |
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Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used as a selective inhibitor of the 20S proteasome.[1],[2],[3] Lactacystin was first characterized by its ability to induce differentiation and inhibit cell cycle progression in several tumor cell lines. At concentrations from 2 to 10 µM, lactacystin induces the outgrowth of neurites in the neuroblastoma cell line Neuro2a.4 Lactacystin irreversibly alkylates subunit X of the 20S proteasome.[3] The concomitant inhibition of proteasome peptidase activity results in the accumulation of a variety of ubiquitinated proteins which would normally undergo rapid degradation. Thus, the effects of lactacystin are pleiotropic and depend substantially on the expression pattern of signalling proteins within the treated cell.
Reference:
[1]. Omura, S., Fujimoto, T.T., Otoguro, K., et al. Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells. Journal of Antibiotics 44, 113-116 (1991).
[2]. Corey, E.J., and Reichard, G.A. Total synthesis of lactacystin. Journal of the American Chemical Society 114, 10677-10678 (1992).
[3]. Fenteany, G., and Schreiber, S.L. Lactacystin, proteasome function, and cell fate. The Journal of Biological Chemisty 273(15), 8545-8548 (1998).
[4]. Fenteany, G., Standaert, R.F., Reichard, G.A., et al. A β-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line. Proceedings of the National Academy of Sciences of the United States of America 91, 3358-3362 (1994).
| Cas No. | 133343-34-7 | SDF | |
| Chemical Name | 2-acetamido-3-[3-hydroxy-2-(1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid | ||
| Canonical SMILES | CC1C(C(NC1=O)(C(C(C)C)O)C(=O)SCC(C(=O)O)NC(=O)C)O | ||
| Formula | C15H24N2O7S | M.Wt | 376.42 |
| Solubility | 1mg/mL in ethanol, 20mg/mL in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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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.
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