Lactacystin

Key inhibitor for use in proteasome research.



BML-PI104-0200	200 µg	120.00 USD

BML-PI104-1000	1 mg	515.00 USD

Replaces Prod. #: ALX-350-260

A potent and selective irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis inhuman monoblast U937 cells. Inhibits NF-κB activation by inhibiting IκB degradation (IC₅₀=10 µM). Inhibits the ubiquitin proteasome pathway in cell culture. Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Formula:	C₁₅H₂₄N₂O₇S

MW:	376.4

Purity:	≥99%

Appearance:	White solid

CAS:	133343-34-7

Source/Host:	Synthetic

Solubility:	Soluble in water (10mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or acetonitrile (20mg/ml)

Long Term Storage:	-20°C

Use/Stability:	Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing aqueous solutons for more than one day.

Handling:	Avoid freeze/thaw cycles. Protect from light.

Background / Technical Information:	Please click here for the comprehensive product datasheet.

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Product Literature References

Proteasome inhibition by lactacystin in primary neuronal cells induces both potentially neuroprotective and pro-apoptotic transcriptional responses: a microarray analysis: E.H. Yew et al.; J. Neurochem. 94, 943 (2005), Abstract;

Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski et al.; Tumour Biol. 22, 211 (2001), Abstract;

Lactacystin activates FLICE (caspase 8) protease and induces apoptosis in Fas-resistant adult T-cell leukemia cell lines: Y. Yamada et al.; Eur. J. Haematol. 64, 315 (2000), Abstract;

Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H.Tomoda & S. Omura ; Yakugaku Zasshi 120, 935 (2000), Abstract;

Lactacystin, a specific inhibitor of the proteasome, induces apoptosis and activates caspase-3 in cultured cerebellar granule cells: L.A. Pasquini et al.; J. Neurosci Res. 59, 601 (2000), Abstract;

Proteasome inhibitors induce cytochrome c-caspase-3-like protease-mediated apoptosis in cultured cortical neurons: J.H. Qiu et al.; J. Neurosci. 20, 259 (2000), Abstract;

Separation of cathepsin A-like enzyme and the proteasome: evidence that lactacystin/beta-lactone is not a specific inhibitor of the proteasome: H. Ostrowska et al.; Int. J. Biochem. Cell. Bio. 32, 747 (2000), Abstract;

Proteasome inhibitors induce mitochondria-independent apoptosis in human glioma cells: H. Kitagawa et al.; FEBS Lett. 443, 181 (1999), Abstract;

Proteasome inhibitors MG132 and lactacystin hyperphosphorylate HSF1 and induce hsp70 and hsp27 expression: D. Kim et al.; Biochem. Biophys. Res. Commun. 254, 264 (1999), Abstract;

Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998), Abstract;

Proteasome inhibitors prevent the degradation of familial Alzheimer’s disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells: P. Marambaud et al.; Mol. Med. 4, 147 (1998), Abstract;

The proteasome inhibitor lactacystin induces apoptosis and sensitizes chemo- and radioresistant human chronic lymphocytic leukaemia lymphocytes to TNF-alpha-initiated apoptosis: J. Delic et al.; Br. J. Cancer 77, 1103 (1998), Abstract;

The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba & C.C. Wang; Mol. Biochem. Parasitol. 93, 11 (1998), Abstract;

Lactacystin and clasto-lactacystin beta-lactone modify multiple proteasome beta-subunits and inhibit intracellular protein degradation and major histocompatibility complex class I antigen presentation: A. Craiu et al.; J. Biol. Chem. 272, 56 (1997), Abstract;

J. Adams and R. Stein; Annual Rep. Med. Chem. 31, 279 (1996),

Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida et al.; Cancer Res. 56, 2945 (1996), Abstract;

Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee et al.; J. Biol. Chem. 271, 25630 (1996), Abstract;

Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu et al.; J Biol Chem 271, 22791 (1996), Abstract;

Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita et al.; Biochem. Biophys. Res. Commun. 224, 74 (1996), Abstract;

Lactacystin increases LDL receptor level on HepG2 cells: H. Miura et al.; Biochem. Biophys. Res. Commun. 227, 684 (1996), Abstract;

Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda et al.; Biochem. Biophys. Res. Commun. 219, 800 (1996), Abstract;

Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami et al.; Biochem. J. 317 ( Pt 1), 77 (1996), Abstract;

Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny et al.; Biochem Biophys Res Commun 227, 564 (1996), Abstract;

M. Katagiri et al.; J. Antibiot. (Tokyo) 48, 334 (1995),

Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori et al.; J. Biol. Chem. 270, 29447 (1995), Abstract;

Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany et al.; Science 268, 726 (1995), Abstract;

Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajoh-Ohmi et al.; Biochem. Biophys. Res. Commun. 217, 1070 (1995), Abstract;

Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka et al.; Biochem. Biophys. Res. Commun. 216, 291 (1995), Abstract;

Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu et al.; J Antibiot (Tokyo) 48, 747 (1995), Abstract;

A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany et al.; PNAS 91, 3358 (1994), Abstract;

Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura et al.; J Antibiot (Tokyo) 44, 113 (1991), Abstract;