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• 产品描述：

  Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

• 靶点： hHDAC3:157 nM (IC50);hHDAC1:198 nM (IC50);hHDAC11:292 nM (IC50);hHDAC6:315 nM (IC50);hHDAC2:325 nM (IC50);hHDAC10:340 nM (IC50);hHDAC7:524 nM (IC50);hHDAC5:532 nM (IC50);hHDAC9:541 nM (IC50);hHDAC8:854 nM (IC50);hHDAC4:1059 nM (IC50);HD1-B:7.5 nM (IC50);HD1-A ;16 nM (IC50);HD2 ;10 nM (IC50);HDAC

• 体内研究：
  Givinostat (ITF2357) at 10 mg/kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg/kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg/kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg

• 参考文献：
  1. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. 2. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. 3. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.101 ml	10.505 ml	21.01 ml
  5 mM	0.42 ml	2.101 ml	4.202 ml
  10 mM	0.21 ml	1.05 ml	2.101 ml
  50 mM	0.042 ml	0.21 ml	0.42 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *