Givinostat hydrochloride monohydrate
| CAS号 | 732302-99-7 | 货号 | BCP02886 |
| 中文名 | Givinostat hydrochloride monohydrate | ||
| 英文名 | Givinostat hydrochloride monohydrate | ||
| 中文别名 | |||
| 英文别名 | Givinostat;ITF 2357;ITF-2357; | ||
| 分子式 | C24H27N3O4.HCl.H2O | 分子量 | 475.97 |
| 生物活性 | 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 decreas | ||
| 信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | HDAC | ||
结构式
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