性能参数

产品名称

Givinostat hydrochloride (ITF-2357 hydrochloride)

规格

2mg 5mg 10mg 50mg 100mg

货号

GOY-Y3785

 含量

>98.00%

CAS

199657-29-9

别名

N/A

化学名

N/A

分子式

C24H28ClN3O4

分子量

分子量 457.95

溶解度

Soluble in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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

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[1]. 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)[2].

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[1].

[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.

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**基乙醛Trimethylacetaldehyde,96%630-19-35ML

3,4,5-**氧基苯甲醛3,4,5-Trimethoxybenzaldehyde,98%86-81-725G

2,4,5-**氧基苯甲醛2,4,5-Trimethoxybenzaldehyde,98%4460-86-05G

2-氯-5-硝基苯甲醛2-Chloro-5-nitrobenzaldehyde,97%6361-21-310G

2-氯乙醛缩二甲醇Chloroacetaldehyde dimethyl acetal,≥99%97-97-225G

3,5-二溴水杨醛3,5-Dibromosalicylaldehyde,98%90-59-510G