426100
Lactacystin
≥99% (HPLC), solid, proteasome inhibitor, Calbiochem®
Synonyma:
Lactacystin, Synthetic, Proteasome Inhibitor VI
Přihlásitk zobrazení cen stanovených pro organizaci a smluvních cen
About This Item
Empirický vzorec (Hillův zápis):
C15H24N2O7S
Číslo CAS:
Molekulová hmotnost:
376.43
UNSPSC Code:
12352200
NACRES:
NA.77
Doporučené produkty
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
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)
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.
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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