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Puromycin Dihydrochloride is the hydrochloride salt form of puromycin, an aminoglycoside antibiotic isolated from the bacterium Streptomyces alboniger. Acting as an analog of the 3' terminal end of aminoacyl-tRNA, puromycin incorporates itself into a growing polypeptide chain and causes its premature termination, thereby inhibiting protein synthesis. This agent has antimicrobial, antitrypanosomal, and antineoplastic properties. Puromycin's main application is in cell biology as a selective antibiotic agent in cell culture systems for selecting mammalian cell lines, which have been transformed by vectors that express puromycin-N-acetyl-transferase (PAC). Puromycin’s longstanding application as a gene selection antibiotic has a powerful new role in Genome editing utilizing the CRISPR/Cas9 system.

Recently researchers have developed a prodrug strategy for selective cancer therapy using a masked cytotoxic agent Fmoc-Lys(Ac)-Puromycin, which can be sequentially activated by histone deacetylases (HDACs) and cathepsin L (CTSL) to kill cancer cells expressing high levels of both enzymes. The data gathered indicates that Fmoc-Lys(Ac)-Puromycin can substantially improve anti cancer efficacy and can be developed into potential selective cancer therapy.

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