J22352 is a potent, highly selective HDAC6 inhibitor with IC50 of 4.7 nM, >2000-fold selective for HDAC6 than for class I HDACs (HDAC1, HDAC2 and HDAC3), and with little activity against HDAC8.
J22352 inhibits glioblastoma cell migration with IC50 of 0.21 uM in Scratch assays for U87MG glioma cells at 24 h.
J22352 induces dose-dependent increase in acetylated α-tubulin expression levels with no increase in the levels of acetylated histone H3 in U87MG glioma cell line.
J22352 exhibits in vitro anti-proliferative activity against U87MG glioma cells with IC50 of 1.56 uM.
J22352 decreases HDAC6 abundance through the proteasomal degradation pathway in cancer cell lines with high expression of HDAC6.
J22352 inhibits autophagosome-lysosome fusion and causes autophagic cancer cell death.
J22352 (10 mg/kg, i.p.) exhibits in vivo efficacy in a glioblastoma xenograft model, enhances the immune response.