PU-11

PU-11 is a Hsp90α/Hsp90β inhibitor with IC₅₀ values of 18.6 μM and 89.8 μM and K_d values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders^[1]. In Vitro:PU-11 (Compound PU-11-trans) (30.1-50.7 μM) binds to purified human Hsp90α NTD with a K_d of 2.0 ± 0.14 μM and an IC₅₀ of 18.6 μM, exhibiting selective affinity for this paralog^[1].
PU-11 (93.3-97.8 μM) binds to purified human Hsp90β NTD with a K_d of 4.2 ± 0.74 μM and an IC₅₀ of 89.8 μM, showing lower affinity than for Hsp90α^[1].
PU-11 (33.0-41.8 μM) binds to purified human Hsp90α^S52A mutant NTD with a K_d of 4.2 ± 0.03 μM, matching its affinity for wild-type Hsp90β^[1].
PU-11 shows IC₅₀ values of 111.4 ± 9.7 and 172.9 ± 7.3 μM for Grp94 and Trap-1^[1].