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Sigma-Aldrich

Lactacystin

≥99% (HPLC), solid, proteasome inhibitor, Calbiochem®

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Synonym(s):
Lactacystin, Synthetic, Proteasome Inhibitor VI
Empirical Formula (Hill Notation):
C15H24N2O7S
CAS Number:
1258004-00-0
Molecular Weight:
376.43
UNSPSC Code:
12352200
NACRES:
NA.77

product name

Lactacystin, Synthetic, Lactacystin, Synthetic, CAS 1258004-00-0, is an irreversible inhibitor of 20S proteasome inhibitor (IC₅₀ = 500 nM). A covalent inhibitor of the chymotrypsin & trypsin-like activities of proteasome.

Quality Level

100

Assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

white

solubility

DMSO: 50 mg/mL
water: soluble

shipped in

ambient

storage temp.

−20°C

General description

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).
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)

Biochem/physiol Actions

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Other Notes

Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol.27, 123.
Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem.31, 279.
Dick, L.R., et al. 1996. J. Biol. Chem.271, 7273.
Oda, K., et al. 1996. Biochem. Biophys. Res.Commun.219, 800.
Fenteany, G., et al. 1995. Science268, 726.
Imajoh-Ohmi, S., et al. 1995. Biochem.Biophys. Res. Commun.217, 1070.
Jensen, T.J., et al. 1995. Cell 83, 129.
Katagiri, M.M., et al. 1995. J. Antibiot.48, 344.
Mori, S., et al. 1995. J. Biol. Chem.270, 29447.
Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun.216, 291.
Fenteany, G., et al. 1994. Proc. Natl. Acad.Sci. USA91, 3358.
Omura, S., et al. 1991. J. Antibiot.44, 117.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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