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Givinostat  99.2509%

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密度：1.259g/ml
包装规格：2mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：Givinostat (ITF-2357) 是 HDAC 抑制剂。抑制 HDAC1 和 HDAC3，IC50 分别为 198 nM 和 157 nM。
溶解性：可溶于 dmso
储备液保存：-80°C, 6 months -20°C, 1 month
靶点：hHDAC3:157nM (IC50);hHDAC1:198nM (IC50);hHDAC11:292nM (IC50);hHDAC6:315nM (IC50);hHDAC2:325nM (IC50);hHDAC10:340nM(IC50) hHDAC7:524nM (IC50);hHDAC5: 532nM (IC50);hHDAC9: 541nM(IC50);hHDAC8:854nM (IC50);hHDAC4:1059nM (IC50);HD1-B:7.5nM (IC50) HD1-A:16nM (IC50);HD2: 10nM(IC50)
体外研究：Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05).
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 (ITF-2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg.
保存条件：2-8°C
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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