| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京