2. Induced Disease Models Products Metabolic Enzyme/Protease Apoptosis
  3. Nervous System Disease Models Proteasome Cathepsin Apoptosis
  4. Parkinson's Disease Models
  5. Lactacystin

Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on[2] [6] .

For research use only. We do not sell to patients.

CAS No. : 133343-34-7

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Based on 8 publication(s) in Google Scholar

Lactacystin Related Antibodies

Top Publications Citing Use of Products

    Lactacystin purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Mar 26.  [Abstract]

    Representative western blots and quantifications of SNCA in R406-treated cultured primary neurons with or without the proteasome inhibitor Lactacystin (4 μM; 24 h) in HEK293 cells.

    Lactacystin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 11:e05479.  [Abstract]

    Immunoblot analysis of extracts of API5−/− A549 cells treated with bafilomycin A1 (BafA1; 200 nm), chloroquine (CQ; 50 μM), 3-methyladenine (3-MA; 10 mm), MG132 (10 μM) or Lactacystin (Lacta; 10 μm) for 6 h followed by infected with SeV for 12 h.

    Lactacystin purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Sep 6;15(9):655.  [Abstract]

    Ishikawa and HEC-1A cells were transfected with Lv-NC or Lv-RAB17. The cells were then treated with the Lactacystin proteasome inhibitor (10 mmol) for 12 h, and Western blot analysis was performed with anti-RAB17 and anti-TFRC antibodies.

    Lactacystin purchased from MedChemExpress. Usage Cited in: iScience. 2023 Feb 27;26(3):106271.

    Western blot analysis for IP3R2 and ERp29 in primary hippocampal neurons transfected with control siRNA (siControl) or ERp29 siRNA for 48h and treated with Lactacystin (0, 10, 20, 40 nM; 48 h) at the indicated dose.

    Lactacystin purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2023;15(2):307-325.  [Abstract]

    Huh7 cells were transfected with CTL-sh or HBP sh1 for 24 hours. Then, the cells were treated with 1 mmol sorafenib and Lactacystin (Lac, 10 mmol) for 12 hours, and immunoblotting was performed with anti-RAF1 and anti-HDLBP antibodies.

    View All Cathepsin Isoform Specific Products:

    View All Isoforms
    Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on[1][2] [3][4][5][6] [7][8][9][10].

    IC50 & Target

    IC50: 4.8 μM (proteasome)[1]
    Cellular Effect
    Cell Line Type Value Description References
    DLD-1 IC50
    0.07 μM
    Compound: Lactacystin
    Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
    Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
    		[PMID: 22206869]
    DLD-1 IC50
    0.3 μM
    Compound: Lactacystin
    Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
    Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
    		[PMID: 22206869]
    MDA-MB-468 IC50
    0.37 μM
    Compound: Lactacystin
    Inhibition of chymotrypsin-like activity of proteasome beta5 subunit in human MDA-MB-468 cells using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 2 hrs by fluorescence assay
    Inhibition of chymotrypsin-like activity of proteasome beta5 subunit in human MDA-MB-468 cells using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 2 hrs by fluorescence assay
    		[PMID: 23547706]
    NCI-H23 IC50
    5.23 μM
    Compound: Lactacystin
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    NCI-H727 IC50
    > 100 μM
    Compound: Lactacystin
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    U-251 IC50
    3481 nM
    Compound: 4
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    		[PMID: 17643112]
    WiDr IC50
    > 10000 nM
    Compound: 4
    Inhibition of SAP130 mediated cell growth in human WiDr cells
    Inhibition of SAP130 mediated cell growth in human WiDr cells
    		[PMID: 17643112]
    In Vitro

    Lactacystin (up to 25.6 µM, 1 h) has no cytotoxicity to HeLa or SH-SY5Y cells, and decreases RVP infection by 63.8% in HeLa and by 74.5% in SH-SY5Y cells[2].
    Lactacystin (2.5 μM) in combination with Parthenolide (HY-N0141) (5 μM) causes a synergistic increase in the apoptotic fraction of the drug-resistant L1210 cells[3].
    Lactacystin (2.5, 5 and 10  µM, 24 h) inhibits the proliferation (IC50 value of 10 μ M) and increases the apoptotic in C6 cells[4].
    Lactacystin (10 μM, 24 h) increases Cisplatin (HY-17394)-induced ER stress-associated apoptosis in Hela cells[5].
    Lactacystin (7.5 μM, 4-48 h) increased reactive oxygen species and GSH levels in HT-29 cells[6].
    Lactacystin (1, 2.5, 5 μM, 24 h) induces stellation in astrocytes from neonatal rat cortex[7].
    Lactacystin (10μM, 8-24 h) induces apoptosis, G2/M cell cycle arrest in the PC12 cells[10].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Lactacystin Related Antibodies

    Cell Viability Assay[4]

    Cell Line: C6 cells
    Concentration: 0, 2.5, 5, 10 µM
    Incubation Time: 24 h
    Result: Suppressed cell growth and viability to 28.9%, and increased the apoptotic in C6 cells.

    Cell Viability Assay[10]

    Cell Line: PC12
    Concentration: 5, 10, 20 µM
    Incubation Time: 24 h
    Result: Declined cell viability in a concentration-dependent manner (79.47% at 5 mM, 49.31% at 10 μM and 31.20% at 20 μM.

    Apoptosis Analysis[10]

    Cell Line: PC12
    Concentration: 10 μM
    Incubation Time: 4, 8, 16, 24h
    Result: Increased significantly apoptotic in a time-dependent manner from 8 to 24 h (14.10% at 8 h, 24.90% at 16 h and 39.41% at 24 h).

    Cell Cycle Analysis[10]

    Cell Line: PC12
    Concentration: 10 μM
    Incubation Time: 4, 8, 16, 24h
    Result: Reduced in the number of cells in the G2-phase (from 17.45% to 30.94%, 31.80% and 32.18%, respectively.) of the cell cycle for 8, 16 and 24h.

    RT-PCR[4][6]

    Cell Line: C6 cells, HT-29 cells
    Concentration: 0, 2.5, 5, and 10 µM (C6 cells）, 7.5 μM in HT-29 cells
    Incubation Time: 24-48 h
    Result: Increased the mRNA in the ratio of Bax to Bcl-2 in C6cells.
    Increased the expression of GGT, GCLC, xCT and Nrf2 in HT-29 cells.

    Western Blot Analysis[4][4]

    Cell Line: C6 cells, HT-29 cells
    Concentration: 0, 2.5, 5, and 10 µM (C6 cells）, 7.5 μM in HT-29 cells
    Incubation Time: 24-48h
    Result: Increased the expression in the ratio of Bax to Bcl-2 in C6cells.
    Increased protein levels of GGT, GCLC, xCT in HT-29 cells.
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Lactacystin (2 μg for ICV) induces a Parkinson’s disease-like motor phenotype 5-7 days after injection in young and adult mice[8].
    Lactacystin (1.0 ug or 5.0? μg/20g for 7days) results in significantly smaller tumor and promotes apoptosis than control in C6 orthotopic xenograft tumor models[4].
    Lactacystin (5 mg/kg/day, dissolved in drinking water, six weeks) induces model of hypertension in male adult Wistar rats[9].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male C57Bl/6RccHsd mice with 8-9 weeks (young) and 12-14 months (adult) old[2]
    Dosage: 2 µg
    Administration: Microinjection
    Result: Induced a Parkinson’s disease-like motor phenotype 5-7 days after injection in young and adult mice.
    Animal Model: Male C57Bl/6RccHsd mice[8]
    Dosage: 2 μg, 7days
    Administration: Intracerebroventricular injection (ICV)
    Result: Induced spontaneous contralateral rotating behavior.
    Animal Model: C6 orthotopic xenograft tumor models[4]
    Dosage: 1.0 µg or 5.0  µg/20g for 7days
    Administration: Intravenous injection (i.p.)
    Result: Reduced the tumor volume.
    Showed polygonal condensed nuclei with brown Tunnel staining indicating apoptosis in tumor tissue.
    Increased the mRNA and protein level in the ratio of Bax to Bcl-2 in tumor tissue.
    Molecular Weight

    376.43

    Formula

    C15H24N2O7S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)[C@H](CSC([C@]([C@@H](O)[C@H]1C)([C@@H](O)C(C)C)NC1=O)=O)NC(C)=O
    Structure Classification
    Initial Source

    Streptomyces OM-6519
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (53.13 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6565 mL 13.2827 mL 26.5654 mL
    5 mM 0.5313 mL 2.6565 mL 5.3131 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 98.24%

    SDS (252 KB)

    COA (256 KB) HNMR (1463 KB) RP-HPLC (291 KB) MS (571 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6565 mL 13.2827 mL 26.5654 mL 66.4134 mL
    5 mM 0.5313 mL 2.6565 mL 5.3131 mL 13.2827 mL
    10 mM 0.2657 mL 1.3283 mL 2.6565 mL 6.6413 mL
    15 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4276 mL
    20 mM 0.1328 mL 0.6641 mL 1.3283 mL 3.3207 mL
    25 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6565 mL
    30 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
    40 mM 0.0664 mL 0.3321 mL 0.6641 mL 1.6603 mL
    50 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
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    Lactacystin Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Lactacystin133343-34-7ProteasomeCathepsinApoptosisL1210C6HelaSHSY-5YHT-29Parkinson’s diseasehypertensionMalariaantiviralanticancerantioxidativeInhibitorinhibitorinhibit

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