Leupeptin

Protease Inhibitor PeptideRx: ResearchCompound: Research

Also known as: Ac-Leu-Leu-Arg-al, Acetyl-leupeptin, Leupeptin, Leupeptin hemisulfate, N-Acetyl-L-leucyl-L-leucyl-L-argininal, N‑acetyl‑L‑leucyl‑L‑leucyl‑L‑argininal

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

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Summary

Leupeptin is a tetrapeptide aldehyde (N‑acetyl‑L‑leucyl‑L‑leucyl‑L‑argininal) that potently inhibits a broad range of proteases and is widely used as a laboratory reagent to prevent proteolysis during protein extraction and purification.

Mechanism of Action

Reversible inhibition of cysteine and serine proteases by forming a covalent hemiacetal with the active‑site nucleophile (aldehyde warhead).

Routes of Administration

In VitroIntraperitoneal

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 clinical use; classified as a research chemical.

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions

What is Leupeptin?

Leupeptin is a tetrapeptide aldehyde (N‑acetyl‑L‑leucyl‑L‑leucyl‑L‑argininal) that potently inhibits a broad range of proteases and is widely used as a laboratory reagent to prevent proteolysis during protein extraction and purification.

What is Leupeptin used for?

Leupeptin is educationally associated with: Experimental neuroprotection model, Autophagy research, Cathepsin inhibition, Calpain inhibition, Protease inhibition in cell lysates. Educational only — not medical advice.

How is Leupeptin administered?

Recorded routes of administration: In Vitro, Intraperitoneal.

What are the potential side effects of Leupeptin?

Reported adverse effects include: Cytotoxicity at high concentrations, Non-specific protease inhibition. This list is not exhaustive — consult a qualified clinician.

Who should avoid Leupeptin?

Recorded contraindications: Human therapeutic use. Consult a qualified clinician before use.