Lactacystin, Synthetic-CAS 1258004-00-0-Calbiochem

C₁₅H₂₄N₂O₇S

376.43

An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC₅₀ = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells beyond theG1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC₅₀ = 10 µM)
An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC₅₀ = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G₁ phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC₅₀ = 10 µM).

Target IC₅₀: 500 nM against 20S proteasome; 10 µM against NF-κB activation
Primary Target
20S proteasome (MCP; multicatalytic proteinase complex)
Product does not compete with ATP.
Reversible: no
Cell permeable: no

Toxicity: Standard Handling (A)

Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H₂O just prior to use.

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Fenteany, G., et al. 1995. Science268, 726.
Imajoh-Ohmi, S., et al. 1995. Biochem.Biophys. Res. Commun.217, 1070.
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CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥99% (HPLC)

solid

Calbiochem^®

OK to freeze

white

DMSO: 50 mg/mL
water: soluble

ambient

−20℃

200, 400 μg in Plastic ampoule
1 mg in Glass bottle

11 - Combustible Solids

WGK 1