HIV-1 Integrase Inhibitor

HIV-1 integrase inhibitor is an inhibitor of HIV-1 integrase strand transfer (IC50s = 0.07 and 0.33 µM in the presence of manganese and magnesium, respectively). It is selective for HIV-1 integrase strand transfer over HIV-1 integrase 3' DNA processing (IC50 = >70 µM in the presence of either manganese or magnesium) and for wild-type HIV-1 integrase over a double-mutant HIV-1 integrase containing F185K and C280S substitutions (HIV-1 integraseF185K/C280S, IC50 = 1.53 µM in the presence of manganese). HIV-1 integrase inhibitor reduces the secreted levels of p24, a marker of HIV-1 replication, in CEM-SS and H9 cells (IC50s = 11 and 7 µM, respectively) without inducing cytotoxicity (CC50s = 600 and 400 µM, respectively).Formal Name: 4-[3-(azidomethyl)phenyl]-2-hydroxy-4-oxo-2-butenoic acid. CAS Number: 544467-07-4. Synonyms: 118-D-24, MA-DKA. Molecular Formula: C11H9N3O4. Formula Weight: 247.2. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: [N-]=[N+]=NCC1=CC(C(C=C(C(O)=O)O)=O)=CC=C1. InChi Code: InChI=1S/C11H9N3O4/c12-14-13-6-7-2-1-3-8(4-7)9(15)5-10(16)11(17)18/h1-5,16H,6H2,(H,17,18). InChi Key: DWAUHOPROZDIJR-UHFFFAOYSA-N.