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Lin28 inhibitor LI71 is an inhibitor of the protein-microRNA precursor interaction between the RNA-binding protein Lin28 and let-7.1 It binds to the cold-shock domain of Lin28 to inhibit let-7 binding and inhibits Lin28-mediated let-7 oligouridylation (IC50 = ~27 µM). Lin28 inhibitor LI71 (100 µM) increases the levels of mature let-7b, -7c, -7f, -7g, and -7i as well as the levels of miR-16, which is not regulated by Lin28, in K562 leukemia cells but not the levels of miR-93, miR-99a, and miR-151, which are also not regulated by Lin28. It increases the levels of mature let-7a-i without increasing miR-16 levels in Lin28a/Lin28b double-knockout mouse embryonic stem cells (mESCs) expressing exogenous wild-type Lin28a. Lin28 inhibitor LI71 also inhibits the protein-protein interaction between P. falciparum cold-shock protein (PfCoSP) and PfDNA or Pfα/β-tubulin.2 It is active against P. falciparum strain 3D7 and the chloroquine-resistant strain RKL-9 (IC50s = 1.35 and 6.3 nM, respectively).
WARNING This product is not for human or veterinary use.
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2. Targeting an essential Plasmodium cold shock protein to block growth and transmission of malaria parasite. iScience 26(5), 106637 (2023).