RI(dl)-2TFA是一种有效的选择性RAD51介导的D环形成(RAD51-mediatedD-loopformation)抑制剂，IC50为11.1μM。RI(dl)-2TFA不会影响RAD51与ssDNA的结合，并会抑制人细胞中的同源重组(HR)活性(IC50为3.0μM)。
RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM)[1].
RI(dl)-2 stabilizes nucleoprotein filaments in a nonfunctional state, which are incapable of D-loop activity and simultaneously shielded from related (e.g., RAD52-mediated) pathways that promote single-strand annealing (SSA)[1].RI(dl)-2 does not modulate the affinity of RAD51 to ssDNA or the stability of preformed RAD51-ssDNA complexes when challenged with high concentrations of salt[1].
[1]. Wei Lv, et al. Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51. J Med Chem. 2016 May 26;59(10):4511-25.
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