Aha1/Hsp90-IN-1

Aha1/Hsp90-IN-1 (Compound 17) is an Aha1/Hsp90 complex inhibitor. Aha1/Hsp90-IN-1 disrupts Aha1/Hsp90 interactions with an IC50 of 3.32 μM. Aha1/Hsp90-IN-1 inhibits tau aggregation[1].

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Research Areas >> Neurological Disease

IC50: 3.32 μM (Aha1/Hsp90 interactions)[1]

Aha1/Hsp90-IN-1 (Compound 17) (10 μM; 24 h) disrupts the Aha1/Hsp90 complex without direct inhibition of Hsp90 protein folding activity[1]. Western Blot Analysis[1] Cell Line: SH-SY5Y neuroblastoma cells and Her2 overexpressing SK-BR-3 breast cancer cells Concentration: 10 μM Incubation Time: 24 h Result: Exhibited the ability to disrupt interactions between Aha1 and Hsp90. Did not induce the degradation of Hsp90 client proteins Her2 (in SK-BR-3 cells), Cdk6, or pAktS473 (in SH SY5Y cells), nor do they induce the expression of Hsp70, a marker of the heat shock response.

[1]. Keegan BM, et al. Synthesis and Evaluation of Small Molecule Disruptors of the Aha1/Hsp90 Complex for the Reduction of Tau Aggregation. ACS Med Chem Lett. 2022 Apr 15;13(5):827-832.