Givinostat (hydrochloride)

Givinostat (hydrochloride) Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

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

• in vitro

  Givinostat (hydrochloride) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduces IL-1β secretion more than 70%. Givinostat suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18.

• in vivo

  Givinostat (ITF2357) at 10 mg/kg is used as a positive control and reduces serum TNFα by 60%. 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.

• target

  hHDAC3 157 nM (IC 50 )

  hHDAC1 198 nM (IC 50 )

  hHDAC11 292 nM (IC 50 )

  hHDAC6 315 nM ( IC 50 )

  hHDAC2 325 nM (IC 50 )

  hHDAC10 340 nM (IC < sub> 50 )

  hHDAC7 524 nM (IC 50 )

  hHDAC5 532 nM (IC 50 )

  hHDAC9 541 nM (IC 50 )

  hHDAC8 854 nM (IC 50 < /sub> )

  hHDAC4 1059 nM (IC 50 )

  HD1-B 7.5 nM (IC 50 )

  HD1-A 16 nM (IC 50 )

  HD2 10 nM (IC 50 )

• Lager

  Store at -20°C

Givinostat (hydrochloride) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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