Art. -Nr.: HY-16594

Lactacystin

8 Cited Publications

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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].

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Reinheit: 99.21%
CAS. Nr.: 133343-34-7
Formel: C₁₅H₂₄N₂O₇S
Molecular Weight:376.43

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lactacystin Chemical Structure

CAS. Nr.: 133343-34-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 4.8 μM (proteasome)^[1]

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 133343-34-7
Appearance Solid
Molecular Weight 376.43
Formel C₁₅H₂₄N₂O₇S
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
- Antibiotics
- Other Antibiotics
Initial Source
- Microorganisms
Streptomyces OM-6519
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (8)

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Journal Impact Factor

Cell Mol Immunol

Oncolytic virus M1 reinvigorates CD8+ T-cell immunity against glioblastoma through B-cell-dependent antigen cross-presentation in the spleen. [Abstract]

2026 Apr;23(4):349-366. PMID: 41781696
Autophagy

R406 and its structural analogs reduce SNCA/α-synuclein levels via autophagic degradation. [Abstract]

2025 Sep;21(9):1945-1961. PMID: 40143425

Lactacystin purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Sep;21(9):1945-1961. [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.
Adv Sci (Weinh)

API5 Phosphorylation Promotes Antiviral Immunity by Inhibiting Degradation of Cytosolic RNA Sensor RLRs. [Abstract]

2025 Jul 11:e05479. PMID: 40641422

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.
Cell Death Dis

RAB17 promotes endometrial cancer progression by inhibiting TFRC-dependent ferroptosis. [Abstract]

2024 Sep 6;15(9):655. PMID: 39242574

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.
Cell Mol Gastroenterol Hepatol

HDLBP promotes hepatocellular carcinoma proliferation and sorafenib resistance by suppressing Trim71-dependent RAF1 degradation. [Abstract]

2023;15(2):307-325. PMID: 36244648

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.
iScience

Non-canonical function of DPP4 promotes cognitive impairment through ERp29-associated mitochondrial calcium overload in diabetes. [Abstract]

2023 Feb 27;26(3):106271. PMID: 36936785

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

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.
Vet Microbiol

The ubiquitin-proteasome system is essential for efficient propagation of Pseudorabies virus. [Abstract]

2025 Aug:307:110602. PMID: 40517584
bioRxiv

2026 Mar 26.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6565 mL

13.2827 mL

26.5654 mL

5 mM

0.5313 mL

2.6565 mL

5.3131 mL

10 mM

0.2657 mL

1.3283 mL

2.6565 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
SDS (252 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Csizmadia V, et al. Effect of proteasome inhibitors with different chemical structures on the ubiquitin-proteasomesystem in vitro. Vet Pathol. 2010 Mar;47(2):358-67. [Content Brief]

[2]. Shaobo Wang, et al. The ubiquitin-proteasome system is essential for the productive entry of Japanese encephalitis virus. Virology. 2016 Nov;498:116-127. [Content Brief]

[3]. Ann H Cory, et al. Lactacystin, a proteasome inhibitor, potentiates the apoptotic effect of parthenolide, an inhibitor of NFkappaB activation, on drug-resistant mouse leukemia L1210 cells. Anticancer Res 2002 Nov-Dec;22(6C):3805-9. [Content Brief]

[4]. Haifeng Wang, et al. The proteasome inhibitor lactacystin exerts its therapeutic effects on glioma via apoptosis: an in vitro and in vivo study. J Int Med Res. 2013 Feb;41(1):72-81. [Content Brief]

[5]. Ye Xu, et al. Proteasome inhibitor lactacystin enhances cisplatin cytotoxicity by increasing endoplasmic reticulum stress-associated apoptosis in HeLa cells. Mol Med Rep. 2015 Jan;11(1):189-95. [Content Brief]

[6]. Nils-Erik Huseby, et al. The proteasome inhibitor lactacystin enhances GSH synthesis capacity by increased expression of antioxidant components in an Nrf2-independent, but p38 MAPK-dependent manner in rat colorectal carcinoma cells. Free Radic Res. 2016;50(1):1-13. https://pubmed.ncbi.nlm.nih.gov/26530909/ [Content Brief]

[7]. Qing-Guo Ren, et al. Lactacystin stimulates stellation of cultured rat cortical astrocytes. Neurochem Res. 2009 May;34(5):859-66. [Content Brief]

[8]. Savolainen MH, et al. Nigral injection of a proteasomal inhibitor, lactacystin, induces widespread glial cell activationand shows various phenotypes of Parkinson's disease in young and adult mouse. Exp Brain Res. 2017 Jul;235(7):2189-2202. [Content Brief]

[9]. Fedor Simko, et al. Lactacystin-Induced Model of Hypertension in Rats: Effects of Melatonin and Captopril. Int J Mol Sci. 2017 Jul 25;18(8):1612. [Content Brief]

[10]. Zhentao Zhang, et al. Cell cycle events mediate lactacystin-induced apoptotic death of neuronal PC12 cells. Cell Biol Int. 2010 Dec;34(12):1181-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Lactacystin

8 Cited Publications

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Lactacystin

Animal Disease Model Inducer Library

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Lactacystin

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lactacystin

Animal Disease Model Inducer Library

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Lactacystin

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lactacystin Related Classifications

HY-16594 Related Classifications