A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC₅₀ = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC₅₀ = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC₅₀ = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC₅₀ >50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
PI4KIIIβ

Reversible: yes

Target IC₅₀: 150 nM for PI4KIII&beta

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20&degC). Stock solutions are stable for up to 3 months at -20°C.

Mejdrova, I., et al. 2015. J. Med. Chem.58, In press.

Spickler, C., et al. 2013. Antimicrob. Agents Chemother.57, 3358.
Sasaki, J., et al. 2012. EMBO J.31, 754.
Arita, M., et al. 2011. J. Virol.85, 2364.

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

Toxicity: Standard Handling (A)