Givinostat hydrochloride,199657-29-9

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YZ剂描述：

产品名称：Givinostat hydrochloride

产品别名：Gavinostat hydrochloride; ITF-2357 hydrochloride

英文别名：Gavinostat hydrochloride;ITF-2357 hydrochloride

靶点：HDAC

CAS：199657-29-9

纯度：0.97

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Givinostat hydrochloride 是 HDAC YZ剂，YZ HDAC1 和 HDAC3，IC50 分别为 198 nM 和 157 nM。

溶解性：10 mM in DMSO

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 (ITF-2357) ≥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 (ITF-2357) ≥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 Givinostat (ITF-2357) 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 ITF3056 (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg.

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