Pracinostat (SB939)

属性

溶解性	DMSO ≥70mg/mL Water <1.2mg/mL Ethanol ≥70mg/mL
存贮条件	储存温度-20°C

描述

应用	A non-selective inhibitor of HDAC.
产品介绍	Pracinostat (SB939)是一种有效的pan-HDAC抑制剂，IC50为40-140 nM，除了HDAC6例外，对III型同工酶SIRT I没有抑制活性。
备注	SB939 is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.
生化机理	SB939 is a potent inhibitor of HDAC class I and II isoenzymes, HDAC1, HDAC2, HDAC3 HDAC4, HDAC5, HDAC7, HDAC8, HDAC9 and HDAC10 with the IC50 values ranging from 43 nM to 140 nM. HDAC6 shows an IC50 of 1008 nM. It markedly inhibits HDAC11 of the HDAC class IV enzymes with an IC50 of 93 nM. SB939 shows significant anti-proliferative activity against a wide variety of tumor cell lines, especially Leukemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells).
别名	SB939; SB-939;(2E)-3-[2-丁基-1-[2-(二乙基氨基)乙基]-1H-苯并咪唑-5-基]-N-羟基丙烯酰胺;SB939; SB-939; SB 939;(2E)-3-[2-Butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl]-N-hydroxyacrylamide