Lin28 Inhibitor LI71

Lin28 inhibitor LI71 is an inhibitor of the protein-microRNA precursor interaction between the RNA-binding protein Lin28 and let-7. 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 Pfalpha/beta-tubulin. It is active against P. falciparum strain 3D7 and the chloroquine-resistant strain RKL-9 (IC50s = 1.35 and 6.3 nM, respectively).Formal Name: 4-[(3aS,4R,9bR)-6-ethoxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl]-benzoic acid. CAS Number: 1357248-83-9. Molecular Formula: C21H21NO3. Formula Weight: 335.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly Soluble: 1-10 mg/mL. SMILES: CCOC1=C2N[C@@H](C3=CC=C(C=C3)C(O)=O)[C@]4([H])[C@](C=CC4)([H])C2=CC=C1. InChi Code: InChI=1S/C21H21NO3/c1-2-25-18-8-4-7-17-15-5-3-6-16(15)19(22-20(17)18)13-9-11-14(12-10-13)21(23)24/h3-5,7-12,15-16,19,22H,2,6H2,1H3,(H,23,24)/t15-,16+,19+/m1/s1. InChi Key: QWJMABCFVYELBB-GJYPPUQNSA-N.