NU7441 (KU-57788) as NHEJ Inhibitors Biological Activity NU7441 selectively inhibits DNA-dependent protein kinase (DNA-PK), a DNA repair enzyme that catalyzes NHEJ, required to repair lethal DSBs. It exhibits ATP-competitive inhibition kinetics, reducing the frequency of NHEJ while increasing the rate of HDR. [1] Target (in cell-free assays) IC50[ 1 ]...
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...
Aphidicolin: Increase HDR via Cell Cycle Synchronization Biological Activity Isolated from the fungus C. aphidicola, aphidicolin is a potent (cell permeable) inhibitor of the B-family of DNA polymerases, (reversibly) arresting replication in eukaryotes, bacteria, and certain animal viruses (SV40, Herpes, Vaccinia) at the G1-S border. Used as a cell synchronization...
Repurposed from a prokaryotic adaptive immune response, the CRISPR/Cas9 system has become a powerful RNA-guided genome-editing tool for targeting and manipulating virtually any genomic sequence, since its inception in 2012. Nowadays CRISPR is being used in a plethora of applications including the elucidation of gene function involved in disease, the...
Polyadenylic acid (also known as poly(A), poly(A) carrier or carrier RNA) is a synthetic homopolymer composed of a long single-stranded (100-500 kDa) sequence of adenine (A) nucleotides available in lyophilized form. Its charge, shape and ability to residue-stack is modulated by solvent composition. It is structurally identical to poly(A) tails,...
Biological Activity For double-stranded DNA (ds-DNA) repair templates, RS-1 stimulates the binding of human HDR protein RAD51 (hRAD51) to cleavage-induced single-stranded DNA (ss-DNA) over-hangs, which enhances HDR proficiency by facilitating the formation of active presynaptic filaments and stabilizing ss-DNA-RAD51 nucleoprotein filaments, without inhibiting hRAD51 ATPase activity. [ 1 ]...