CAS: 1454619-13-6

PU-H54

PU-H54 is a purine-derived Grp94 inhibitor targeting the S2 subpocket's unique binding region.

PU-H54 is a chaperone that has potent inhibitory activity against the formation of aggregates of proteins in the endoplasmic reticulum. It also has anti-inflammatory properties and is able to inhibit pro-inflammatory cytokines, such as TNF-α, IL-1β and IL-6. PU-H54 is able to inhibit the growth of cancer cells by inhibiting protein aggregation and may be used for the treatment of autoimmune diseases. This agent also has pharmacokinetic properties that make it suitable for intravenous administration. The low energy required for PU-H54 to bind with other molecules makes this drug a good candidate for chemical biology applications. PU-H54 binds with an affinity constant (K) of around 0.5 nM to human Hsp70 and Hsp90, which are molecular chaperones found in cells that help maintain protein homeostasis during stress conditions. Structural analysis has shown that PU-H54 binds to