- Home
- Signaling Pathways
- Ubiquitination/ Proteasome
- Proteasome
- Lactacystin (Synthetic)
Lactacystin (Synthetic)
Lactacystin is a specific and an irreversible inhibitor of proteasome with IC50 value of 4.8 μM [1].
Lactacystin binds to the catalytic subunits of the 20 S proteasome and inhibits all the three peptidase activities of the proteasome, chymotrypsin-like, trypsin-like and caspase-like. With this feature, lactacystin is used to study the role of the proteasome. In Neuro-2a cells, lactacystin treatment resulted in the induction of neurite outgrowth. It caused a transient increase in cAMP levels and the bipolar morphology of the cells. Lactacystin also inhibited cell cycle progression in MG-63 human osteosarcoma cells. Moreover, lactacystin was reported to have therapeutic effects on glioma cells. In rat C6 glioma cells, lactacystin significantly inhibited cell growth with IC50 value of about 10 μM. Besides that, in a mouse gliomaxenograft model, administration of lactacystin resulted in tumor size reduction at a dose of 1-5 μg / 20 g body weight [2, 3].
References:
1.?Csizmadia V, Csizmadia E, Silverman L, et al. Effect of proteasome inhibitors with different chemical structures on the ubiquitin–proteasome system in vitro. Veterinary Pathology Online, 2010, 47(2): 358-367.
2.?Fenteany G, Schreiber S L. Lactacystin, proteasome function, and cell fate. Journal of Biological Chemistry, 1998, 273(15): 8545-8548.
3.?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.
- 1. Lifang Zou, Xia Yu, et al. "Partial Replacement of NaCl with KCl in Cooked Meat Could Reduce the Liver Damage Through Renin–Angiotensin System in Mice." Mol Nutr Food Res. 2024 Feb;68(4):e2200783. PMID: 38308101
- 2. Xiaozhou Li, Ye Yang, et al. "Chitosan hydrogel loaded with recombinant protein containing epitope C from HSP90 of Candida albicans induces protective immune responses against systemic candidiasis." Int J Biol Macromol. 2021 Mar 15;173:327-340. PMID:33482211
- 3. Yunkai Yang, Xiaohan Guo, et al. "Generated SecPen_NY-ESO-1_ubiquitin-pulsed dendritic cell cancer vaccine elicits stronger and specific T cell immune responses." Acta Pharmaceutica Sinica B Available online 25 August 2020.
- 4. Mukhopadhyay U, Chanda S, et al. "Bi-phasic regulation of RNA interference during Rotavirus infection by modulation of Argonaute2." Cell Microbiol. 2019 Aug 19:e13101. PMID:31424151
- 5. Zheng Y, Liu Q, t al. "Zika virus elicits inflammation to evade antiviral response by cleaving cGAS via NS1-caspase-1 axis." EMBO J. 2018 Jul 31. pii: e99347. PMID:30065070
| Storage | Store at -20°C |
| M.Wt | 376.42 |
| Cas No. | 133343-34-7 |
| Formula | C15H24N2O7S |
| Solubility | Soluble in H2O |
| Chemical Name | 2-acetamido-3-[3-hydroxy-2-(1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1C(C(NC1=O)(C(C(C)C)O)C(=O)SCC(C(=O)O)NC(=O)C)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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. |
|
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
Related Biological Data
