Givinostat hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Givinostat Hydrochronide 是一种 HDAC 抑制剂，对 HDAC1 和 HDAC3 的 IC50 分别为 198 和 157 nM。 Givinostat 盐酸盐具有抗炎、抗血管生成和抗肿瘤活性。

Givinostat hydrochloride is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.(In Vitro):Givinostat hydrochloride inhibits JS-1 cell proliferation in a concentration-dependent manner. Givinostat hydrochloride (≥500 nM) is associated with significant inhibition of JS-1 cell proliferation. Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat hydrochloride ≥250 nM plus LPS and the group without LPS treatment. Givinostat hydrochloride (25, 50, and 100 nM) reduces IL-1β secretion more than 70%. Givinostat hydrochloride 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, but at 100 and 200 nM, there is no reduction.(In Vivo):Givinostat hydrochloride (10 mg/kg) reduces serum TNFα by 60%. Pretreatment of Givinostat hydrochloride (0.1 mg/kg) significantly reduces the circulating TNFα by nearly 90%.

Givinostat (ITF2357) 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. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction. Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner in the CCK-8 assay. Treatment with Givinostat (ITF-2357) ≥500 nM is associated with significant inhibition of JS-1 cell proliferation. 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.

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.

Givinostat HCl | ITF2357 | ITF-2357 | ITF 2357 | ITF2357 HCl | ITF2357 hydrochloride

Cell Cycle/DNA Damage

HDAC

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199657-29-9

457.96

C24H28ClN3O4

>98% (HPLC)

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Cl.CCN(CC)Cc1ccc2cc(COC(=O)Nc3ccc(cc3)C(=O)NO)ccc2c1

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(-20℃)

With Ice Pack

≥ 2 years