HIV TAR Hairpin Binder

A cell-permeable, non-cationic thienopyridine compound that selectively targets HIV-1 transactivation response (TAR) hairpin motif (K_d = 2.4 µM), but not other structural elements in HIV-1 5′ untranslated region (UTR), via hydrophobic & aromatic type of interactions, reducing TAR conformational flexibility without affecting UTR dimerization. Shown to protect T-lymphoblastoid cell line CEM-SS against HIV-1-induced cytopathicity (% cell survival/[drug] in µM = 90%/550, 78%/167, 50%/28 in 6-d infected cultures by XTT) without conferring cytotoxicity in non-infected cultures even at concentrations as high as 550 µM.

A cell-permeable, non-cytotoxic, non cationic thienopyridine compound that potently and dose-dependently inhibits HIV-mediated cytopathicity (EC₅₀ = 28 µM in T lymphocytes) and displays antiviral properties. Shown to specifically bind and stabilize HIV transactivation response (TAR) element RNA hairpin motif (K_d = 2.4 µM) in a reversible manner without disrupting 5′ untranslated region (UTR).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
HIV transactivation response (TAR) element RNA

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sztuba-Solinska, J., et al. 2014. J. Am. Chem. Soc.136, 8402.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)