2. Induced Disease Models Products Metabolic Enzyme/Protease Apoptosis Protein Tyrosine Kinase/RTK
  3. Nervous System Disease Models Proteasome Apoptosis ROS Kinase
  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[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .

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

Lactacystin Chemical Structure

Lactacystin Chemical Structure

CAS No. : 133343-34-7

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Based on 3 publication(s) in Google Scholar

Lactacystin Related Antibodies

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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]
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 (10μM, 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

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 ug 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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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 98.2%

COA (256 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

Help & FAQs
  • 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:

Lactacystin133343-34-7ProteasomeApoptosisROS KinaseL1210C6HelaSHSY-5YHT-29Parkinson’s diseasehypertensionMalariaantiviralanticancerantioxidativeInhibitorinhibitorinhibit

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