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AZT as HDR Inhibitors
Biological Activity
Approved by the FDA in 1987,[1] and still used in combination treatment, azidothymidine (AZT) is a thymidine (nucleoside) analogue that is phosphorylated in the host (by enzymes of the thymidine-phosphorylation pathway) to AZT-triphosphate, which inhibits viral (HIV-1) reverse transcriptase activity about 100-fold better than cellular polymerase α. [1,2,3] AZT was also found to decrease CRISPR/Cas9-mediated HDR outcomes. [4]
Successful Applications in CRISPR
AZT decreased the HDR efficiency in mouse embryonic stem cells (ESCs) by 3-fold or by more than 10-fold as detected by flow cytometry or sequencing respectively. At AZT’s optimal concentration of 5 μM, no or very mild toxicity was observed, and optimal activity was achieved within the first 24-hour window postelectroporation.
Moreover, AZT increased the knockout efficiency (in the absence of a donor template) in a clonal mouse ESC line. For example, in the case of sgGFP-1, the knockout efficiency increased by more than 1.8-fold.[ 4 ]
Reference:
Related Product:
431574 3'-Azido-3'-deoxythymidine(Zidovudine), 98% [CAS: 30516-87-1]