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426100 Lactacystin, Synthetic - CAS 1258004-00-0 - Calbiochem

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

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Synonyms: Proteasome Inhibitor VI

Primary Target: 20S proteasome (MCP; multicatalytic proteinase complex)
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426100
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Overview

Key Spec Table

CAS #Empirical Formula
1258004-00-0C₁₅H₂₄N₂O₇S

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426100-1MGCN
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      426100-200UGCN
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          426100-400UGCN
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              Description
              OverviewAn 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).
              Catalogue Number426100
              Brand Family Calbiochem®
              SynonymsProteasome Inhibitor VI
              References
              ReferencesKeyomarsi, 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. Science 268, 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. USA 91, 3358.
              Omura, S., et al. 1991. J. Antibiot. 44, 117.
              Product Information
              CAS number1258004-00-0
              ATP CompetitiveN
              FormWhite solid
              Hill FormulaC₁₅H₂₄N₂O₇S
              Chemical formulaC₁₅H₂₄N₂O₇S
              ReversibleN
              Structure formula ImageStructure formula Image
              Quality LevelMQ100
              Biological Information
              Primary Target20S proteasome (MCP; multicatalytic proteinase complex)
              Primary Target IC<sub>50</sub>500 nM against 20S proteasome; 10 µM against NF-κB activation
              Purity≥99% by HPLC
              Physicochemical Information
              Cell permeableN
              Storage and Shipping Information
              Ship Code Ambient Temperature Only
              Toxicity Standard Handling
              Storage -20°C
              Do not freeze Ok to freeze
              Special InstructionsFollowing 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.
              Global Trade Item Number
              Catalogue Number GTIN
              426100-1MGCN 04055977187311
              426100-200UGCN 04055977187328
              426100-400UGCN 04055977187335