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Givinostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Givinostat图片
CAS NO:497833-27-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ITF-2357
产品介绍
Givinostat (ITF-2357) 是HDAC抑制剂。抑制HDAC1HDAC3IC50分别为 198 nM 和 157 nM。
生物活性

Givinostat (ITF-2357) is aHDACinhibitor with anIC50of 198 and 157 nM forHDAC1andHDAC3, respectively.

IC50& Target[1][3]

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)

体外研究
(In Vitro)

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 ≥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)[2].

体内研究
(In Vivo)

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[1].

Clinical Trial
分子量

421.49

Formula

C24H27N3O4

CAS 号

497833-27-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.