中文名：Givinostat (ITF2357)
英文名：Givinostat (ITF2357)
英文別名：(6-((diethylamino)methyl)naphthalen-2-yl)methyl 4-(hydroxycarbamoyl)phenylcarbamate hydrochloride hydrate
純度：10mM in DMSO
貨號(hào)：G407983
包裝：1ml
Cas號(hào)：732302-99-7
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
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%
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對(duì)應(yīng)頁面：https://www.aladdin-e.com/zh_cn/G407983.html
關(guān)鍵字： (6-((diethylamino)methyl)naphthalen-2-yl)methyl 4-(hydroxycarbamoyl)phenylcarbamate hydrochloride hydrate
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代碼：688179），專注于科研試劑的研發(fā)、生產(chǎn)和銷售，已陸續(xù)建立多個(gè)工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅(jiān)持質(zhì)量第一，連續(xù)13年被評(píng)為“最受歡迎試劑品牌”。
阿拉丁目前常備庫存試劑產(chǎn)品品種超過7萬種，SKU總數(shù)超過46萬，產(chǎn)品線涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個(gè)領(lǐng)域，是國內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國內(nèi)（www.aladdin-e.com）和海外（www.aladdinsci.com）電商平臺(tái)。