N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐

中文名称： N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐

英文名称： Tubastatin A HCl

CAS： 1310693-92-5

分子式： C₂₀H₂₁N₃O₂.HCl

分子量： 372

EINECS号：

中文同义词 N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐英文同义词

Tubastatin A HCl

基本性质

熔点	>221°C (subl.)
溶解度	Soluble in DMSO or Water.
形态	powder
颜色	white to tan

安全信息

WGK Germany	3
危险性描述	H315-H319
海关编码	29339900

CHS信息

危险性符号(GHS)	GHS07
警示词	Warning
防范说明	P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

生产方法及用途

用途	一种高效、选择性的HDAC6抑制剂,IC50:15nM。Tubastatin A demonstrates 1093-fold selectivity over HDAC1 (IC50 values of 15 nM for HDAC6 vs 16.4 ?μM for HDAC1). Tubastatin A was substantially more selective than the known HDAC6 inhibitor Tubacin at all isozymes except HDAC8. Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. Comparatively, it demonstrates over 1,000-fold selectivity against all other HDAC isoforms (IC50 >16 μM), excluding HDAC8 (IC50= 0.9 μM). Tubastatin A induces α-tubulin hyperacetylation at 2.5 μM in primary cortical neuron cultures. In a model of oxidative stress induced by glutathione depletion, tubastatin A displays dose-dependent neuronal protection of primary cortical neuron cultures at 5-10 μM.

用途

一种高效、选择性的HDAC6抑制剂,IC50:15nM。Tubastatin A demonstrates 1093-fold selectivity over HDAC1 (IC50 values of 15 nM for HDAC6 vs 16.4 ?μM for HDAC1). Tubastatin A was substantially more selective than the known HDAC6 inhibitor Tubacin at all isozymes except HDAC8. Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. Comparatively, it demonstrates over 1,000-fold selectivity against all other HDAC isoforms (IC50 >16 μM), excluding HDAC8 (IC50= 0.9 μM). Tubastatin A induces α-tubulin hyperacetylation at 2.5 μM in primary cortical neuron cultures. In a model of oxidative stress induced by glutathione depletion, tubastatin A displays dose-dependent neuronal protection of primary cortical neuron cultures at 5-10 μM.