MHY219

MHY219 is a histone deacetylase (HDAC) inhibitor with an IC₅₀ of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer^[1]. In Vitro:MHY219 (0.001-10 μM; 30 min) potently inhibits total HDAC enzyme activity with an IC₅₀ of 0.276 μM in a cell-free fluorometric assay^[1].
MHY219 (0.05-5 μM; 24-48 h) inhibits the proliferation of DU145, LNCaP, and PC3 human prostate cancer cells with 48 h IC₅₀ values of 0.36 μM, 0.97 μM, and 5.12 μM, respectively, and induces morphological changes in DU145 cells^[1].
MHY219 (0.1-1 μM; 48 h) increases histone H3 and H4 hyperacetylation and down-regulates specific class I and II HDAC subtypes in DU145, LNCaP, and PC3 human prostate cancer cells^[1].
MHY219 (0.1-1 μM; 48 h) induces sub-G1 accumulation and G2/M phase arrest in DU145 cells, G1 phase arrest in LNCaP cells, and G2/M phase arrest in PC3 cells, with corresponding changes in cell cycle regulatory protein expression^[1].
MHY219 (0.1-1 μM; 24-48 h) induces apoptosis in DU145 human prostate cancer cells via a mitochondria-mediated pathway, but does not induce apoptosis in LNCaP or PC3 cells^[1].
MHY219 (0.5-1 μM; 48 h) increases androgen receptor expression in DU145 human prostate cancer cells, but does not affect AR expression in LNCaP or PC3 cells^[1].