CA-074 methyl ester

Summary

CA-074 methyl ester (CA-074 Me) is a cell-permeable prodrug form of the cathepsin B inhibitor CA-074. It is widely used as a biochemical tool compound in cell-based research to selectively inhibit cathepsin B activity intracellularly. It has been applied in studies of lysosomal pathways, apoptosis, neurodegeneration, inflammation, and cancer biology. It has no approved clinical indication and is used exclusively as a research reagent.

Mechanism of Action

Selective, cell-permeable inhibitor of cathepsin B; the methyl ester prodrug form is hydrolyzed intracellularly to the active CA-074, which irreversibly or pseudo-irreversibly inhibits cathepsin B by blocking its active-site cysteine, thereby suppressing lysosomal cysteine protease-mediated protein degradation and downstream signaling pathways including NLRP3 inflammasome activation.

Routes of Administration

Goals & Uses

• Apoptosis and autophagy pathway researchCell Biology ResearchModerate
• Cancer biology researchOncology ResearchModerate
• Neuroprotection researchNeuroscience ResearchModerate
• NLRP3 inflammasome suppressionInflammation ResearchModerate
• Cathepsin B inhibition (in vitro/in vivo research)Research Tool / Enzyme InhibitionHigh

Contraindications

• Human therapeutic useRegulatory/safetyHigh

Adverse Effects

• Cytotoxicity at high concentrationsIn Vitro ToxicityUncommon
• Off-target protease inhibitionPharmacologicalRare

Drug Interactions

No drug interactions recorded yet.

Population Constraints

• Not for human administrationGeneral PopulationAbsolute

Regulatory Status

• European UnionUnapprovedResearch reagent only; not reviewed by EMA.
• United StatesUnapprovedResearch reagent only; not reviewed by FDA for any therapeutic indication.
• United KingdomUnapprovedResearch reagent only; not reviewed by MHRA.

Not approved for human therapeutic use in any jurisdiction. Available only as a research chemical/reagent. Not regulated as a pharmaceutical drug.

Evidence & Sources

No sources recorded yet.