Lactacystin (Synthetic) |
カタログ番号GC13123 |
20Sプロテアソームの選択的阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133343-34-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
C6 cells |
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. |
Reacting condition |
2.5, 5 or 10 μM |
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]: | |
Animal models |
Nude mice bearing gliomas |
Dosage form |
1.0 μg or 5.0 μg per 20 g body weight; i.p.; q.d., for 7 days |
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. |
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. |
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. |
ラクタシスチンは、ストレプトマイセスから分離された微生物代謝産物であり、現在は広く20Sプロテアソームの選択的阻害剤として使用されています[1] [2] [3]。ラクタシスチンは最初に、いくつかの腫瘍細胞株で分化を誘導し、細胞周期進行を阻害する能力によって特徴付けられました。濃度が2〜10μMの場合、ラクタシスチンは神経芽腫細胞株Neuro2aでニューライトの発育を誘導します[4]。ラクタシスチンは20SプロテアソームサブユニットXを不可逆的にアルキル化します[3]。同時にプロテアソームペプチダーゼ活性が阻害されることで、通常迅速な分解が起こる多様なユビキチン化されたタンパク質が蓄積します。したがって、ラクタシスチンの効果はpleiotropicであり、処理された細胞内の信号伝達タンパク質の発現パターンに大きく依存します。
References:
[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 |
溶解度 | 1mg/mL in ethanol, 20mg/mL in DMSO, or in DMF | 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. |
||
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 | 2.6566 mL | 13.283 mL | 26.5661 mL |
5 mM | 0.5313 mL | 2.6566 mL | 5.3132 mL |
10 mM | 0.2657 mL | 1.3283 mL | 2.6566 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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