中文名：Givinostat (ITF2357)
英文名：Givinostat (ITF2357)
英文别名：(6-((diethylamino)methyl)naphthalen-2-yl)methyl 4-(hydroxycarbamoyl)phenylcarbamate hydrochloride hydrate
纯度：10mM in DMSO
货号：G407983
包装：1ml
Cas号：732302-99-7
存储温度：-80℃储存
产品介绍：
Information
Givinostat (ITF2357) is a potentHDACinhibitor for maize HD2, HD1B and HD1A withIC50of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.
In vitro
In LPS-stimulated cultured human peripheral blood mononuclear cells (PBMCs), ITF2357 reduces the release of TNFα, IL-1α, IL-1β, and IFNγ, with IC50 of 10-25 nM, respectively. Using the combination of IL-12 plus IL-18, ITF2357 reduces IFNγ and IL-6 production with IC50 of 12.5-25 nM, independent of decreased IL-1 or TNFα. ITF2357 is cytotoxic in multiple myeloma (MM) cell lines (RPMI8226, NCI-H929, JJN3, KMS 11, KMS 12, KMS 18, and KMS 20) and acute myelogenous leukemia (AML) cell lines (HL-60, THP-1, U937, KASUMI, KG-1, and TF-1), with IC50 of 200 nM. ITF2357 activates the intrinsic apoptotic pathway, upregulates p21 and downmodulates Bcl-2 and Mcl-1. ITF2357 inhibits the production of IL-6, VEGF, and IFNγ in mesenchymal stromal cells (MSCs) by 80-95%. ITF2357 favors β-cell survival during inflammatory conditions. ITF2357 at concentrations of 25 and 250 nM increases islet cell viability, enhances insulin secretion, inhibits release of MIP-1α and MIP-2, reduces NO production and decreases apoptosis rates.
In vivo
ITF2357 (1-10 mg/kg) reduces LPS-induced serum TNFα and IFNγ by more than 50% in mice. Anti-CD3-induced cytokines are not suppressed by ITF2357 in PBMCs in the circulation in mice. In concanavalin-A-induced hepatitis, ITF2357 (1 or 5 mg/kg) significantly reduces liver damage. ITF2357 (10 mg/kg) significantly prolongs survival of severe combined immunodeficient mice inoculated with the AML-PS in vivo passaged cell line. In a mouse model of closed head injury (CHI), ITF2357 (10 mg/kg) improves neurobehavioral recovery, decreases neuronal degeneration, reduces lesion volume, and induces glial apoptosis.
Cell Data
cell lines：
Concentrations：1 nM - 1 μM
Incubation Time：24 hours
Powder Purity:≥95%
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关键字： (6-((diethylamino)methyl)naphthalen-2-yl)methyl 4-(hydroxycarbamoyl)phenylcarbamate hydrochloride hydrate
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