KT-531
CAS号 | 2490284-18-7 | 货号 | BCP48476 |
中文名 | KT-531 | ||
英文名 | KT-531 | ||
中文别名 | |||
英文别名 | KT531;KT 531; | ||
分子式 | C17H14F4N2O4S | 分子量 | 418.36 |
生物活性 | KT-531 is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms;KT-531 demonstrated biological potency in multiple hematological cancer cell models (acute myeloid leukemia (AML), PTCL, and T-cell acute lymphoblastic leukemia (T-ALL)) and limited cytotoxicity in nonmalignant cell types as well as no observable toxicity in vivo (CD-1 mice).KT-531 exhibited strong potency (IC50=0.42 μM) in the T-ALL/T-PLL-like cell line SUP-T11, demonstrated higher cytotoxicity than Nexturastat in MV4-11 cancer cells (IC50=0.42 uM versus 1.68 uM).KT-531 showed high synergy with chemotherapeutic agents idasanutlin, bendamustine, and venetoclax in T-PLL patient samples.KT-531 is the first HDAC6 inhibitor to show efficacy in T-PLL patient samples. | ||
信号通路 | Cell Cycle/DNA Damage | ||
靶 点 | HDAC |
结构式
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