HDAC6-IN-87

HDAC6-IN-87 (compound 27) is a potent and selective HDAC6 inhibitor with an IC₅₀ of 4.29 nM; for HDAC1 IC₅₀ = 749.59 nM, HDAC3 IC₅₀ = 813.09 nM, HDAC8 IC₅₀ >1000 nM, HDAC10 IC₅₀ = 679.25 nM, and HDAC11 IC₅₀ >1000 nM^[1].
HDAC6-IN-87 (0.1-2.5 μM; 48 h) preferentially targets HDAC6 in a cellular context, as evidenced by dose-dependent upregulation of the HDAC6 substrate acetylated α-tubulin without significantly affecting the Class I HDAC substrate acetylated histone H3^[1].
HDAC6-IN-87 (molecular docking and molecular dynamics simulation) is predicted to bind to the HDAC6 active site; it forms hydrogen bonds with H611, G619, and Y782, π-π stacking with F620, H651, F679, and F680, and hydrophobic contacts with D567, S568, H610, C618, C621, P681, M682, and L749^[1].
HDAC6-IN-87 (48 h) exhibits broad-spectrum anticancer potential, demonstrating antiproliferative activity against HCT-116 (IC₅₀ = 0.69 μM), HL60 (IC₅₀ = 3.65 μM), A375 (IC₅₀ = 3.65 μM), MDA-MB-231 (IC₅₀ = 5.37 μM), and A549 (IC₅₀ = 6.72 μM) cells^[1].
HDAC6-IN-87 (0.25-1.0 μM; 48 h) significantly disrupts cell cycle progression and primarily induces G₂/M phase arrest in HCT-116 cells; it induces apoptosis in HCT-116 cells by inducing late apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.