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Lactacystin (Synthetic)

In stock
Catalog No.
A2583
Proteasome inhibitor
Grouped product items
SizePriceStock Qty
100ug
$86.00
In stock
500ug
$365.00
In stock
1mg
$638.00
In stock

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Background

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.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt376.42
Cas No.133343-34-7
FormulaC15H24N2O7S
SolubilitySoluble in H2O
Chemical Name2-acetamido-3-[3-hydroxy-2-(1-hydroxy-2-methylpropyl)-4-methyl-5-oxopyrrolidine-2-carbonyl]sulfanylpropanoic acid
SDFDownload SDF
Canonical SMILESCC1C(C(NC1=O)(C(C(C)C)O)C(=O)SCC(C(=O)O)NC(=O)C)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Protocol

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

Quality Control & MSDS

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Chemical structure

Lactacystin (Synthetic)

Related Biological Data

Lactacystin (Synthetic)