HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor targeting HDAC6 and Hsp90, exhibiting IC50 values of 105.7 nM and 61 nM, respectively. It is primarily utilized in cancer research [1].

HDAC6/HSP90-IN-2 (compound 6e) (0.05-2 μM; 24 h) effects HSP90, HDAC6 and signaling pathways regulated by Hsp90 dose-dependently [1]. HDAC6/HSP90-IN-2 (compound 6e) (2 μM; 24 h) promotes the acetylation of HSP90 [1]. HDAC6/HSP90-IN-2 (compound 6e) (0-100 μM; 24-72 h) inhibits the growth of H1975 non-small cell lung cancer cells [1]. HDAC6/HSP90-IN-2 (compound 6e) (0-2 μM; 24 h) induces apoptosis of H1975 cells [1]. Western Blot Analysis [1] Cell Line: H1975 cells Concentration: 0.05, 0.1, 0.5, 1 and 2 μM Incubation Time: 24 hours Result: Showed inhibitory effect to Hsp90 and HDACs dose-dependently and increased the expression levels of Hsp70 and Hsp90 probably by activates HSF1. Western Blot Analysis [1] Cell Line: H1975 cells Concentration: 2 μM Incubation Time: 24 hours Result: Promoted the acetylation of Hsp90 by inhibiting HDAC6, and increased the acetylation at K294 residue of Hsp90. Apoptosis Analysis [1] Cell Line: H1975 cells Concentration: 0, 0.5, 1 and 2 μM Incubation Time: 24 hours Result: Induced early and late apoptosis of H1975 cells dose-dependently. Cell Viability Assay [1] Cell Line: H1975 cells Concentration: 0-100 μM Incubation Time: 24, 48 and 72 h Result: Inhibited the growth of H1975 non-small cell lung cancer cells with a GI 50 value of 1.7 μM.

HDAC6/HSP90-IN-2 (compound 6e) (25-50 mg/kg; i.p. every weekdays for 6 weeks) exhibits antitumor activity of in NOD-scid IL2Rgammanull (NSG) mice with xenotransplantation of H1975 cells [1]. Animal Model: NOD-scid IL2Rgammanull (NSG) mouse with H1975 cells xenograft [1] Dosage: 25-50 mg/kg Administration: Intraperitoneal injection; 25-50 mg/kg for every weekdays; for 6 weeks Result: Delayed tumor growth after 2 weeks and reduced the growth rates of tumors in mice.