Leupeptin
Also known as: Ac-Leu-Leu-Arg-al, Acetyl-leupeptin, Leupeptin hemisulfate, N-Acetyl-L-leucyl-L-leucyl-L-argininal
Summary
Leupeptin is a naturally occurring tripeptide aldehyde (Ac-Leu-Leu-Arg-al) produced by Streptomyces species. It is a potent, reversible inhibitor of serine and cysteine proteases and is widely used as a research tool in cell biology and biochemistry to prevent proteolytic degradation in cell lysates and experimental assays. It has no approved clinical use.
Mechanism of Action
Reversible inhibitor of serine and cysteine proteases; acetylates the active site of target enzymes such as trypsin, plasmin, thrombin, papain, cathepsins, and calpains by forming a hemiacetal or thiohemiacetal with the catalytic serine or cysteine residue.
Routes of Administration
Goals & Uses
- Experimental neuroprotection modelPreclinical ResearchLow
- Autophagy researchResearch ToolHigh
- Cathepsin inhibitionResearch ToolHigh
- Calpain inhibitionResearch ToolHigh
- Protease inhibition in cell lysatesResearch/biochemistryHigh
Contraindications
- Human therapeutic useRegulatory/safetyHigh
Adverse Effects
- Cytotoxicity at high concentrationsIn Vitro ToxicityUncommon
- Non-specific protease inhibitionOff Target EffectCommon
Drug Interactions
- E-64 / E64dLow
- PMSF (phenylmethylsulfonyl fluoride)Low
Population Constraints
- All human populationsGeneralAbsolute
Regulatory Status
- European UnionUnapprovedNo EMA approval; available only as a research chemical.
- United StatesUnapprovedResearch reagent only; no FDA approval or IND filing on record.
- United KingdomUnapprovedNo MHRA approval; research use only.
Not approved for human therapeutic use in any jurisdiction. Sold exclusively as a research-grade reagent. No IND or clinical trials on record for therapeutic application.
Evidence & Sources
No sources recorded yet.