Givinostat

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Givinostat

CAS No. : 497833-27-9

MCE 国际站：Givinostat

产品活性：Givinostat (ITF-2357) 是 HDAC 抑制剂。抑制 HDAC1 和 HDAC3，IC₅₀ 分别为 198 nM 和 157 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

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. 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).

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.

相关产品：Trichostatin A  |  Vorinostat  |  4-Phenylbutyric acid  |  Valproic acid  |  Sulforaphane  |  Panobinostat  |  Entinostat  |  Romidepsin  |  Tucidinostat  |  RGFP966  |  Belinostat  |  Ricolinostat  |  Tubastatin A  |  TMP195  |  Theophylline  |  Carbamazepine  |  Mocetinostat  |  Santacruzamate A  |  ITSA-1  |  TMP269  |  Tasquinimod  |  Fimepinostat  |  Tubacin  |  LMK-235  |  Quisinostat  |  PCI-34051  |  FT895

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds