• 欢迎来到美国APExBIO中文站,专注小分子抑制剂、激动剂、拮抗剂及化合物库!

 


加 微 信 得 红 包
ApexBio
Search Site
首页 >> Signaling Pathways >> DNA Damage/DNA Repair >> HDAC >> ITF2357 (Givinostat)
相关产品
ITF2357 (Givinostat)HDAC抑制剂

ITF2357 (Givinostat)

产品编号:A4093
ApexBio 的所有产品仅用作科研,我们不为任何个人用途提供产品和服务
规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥1,200.00 现货
5mg ¥1,100.00 现货
10mg ¥1,900.00 现货
50mg ¥6,700.00 现货
200mg ¥14,800.00 现货

电话: 021-55669583

Email: sales@apexbio.cn

全球经销商

Sample solution is provided at 25 µL, 10mM.

引用文献

1.Topper MJ, Vaz M, et al. "Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer." Cell. 2017 Nov 30;171(6):1284-1300.e21. PMID:29195073
2.Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187

质量控制

化学结构

ITF2357 (Givinostat)

相关生物数据

ITF2357 (Givinostat)

相关生物数据

ITF2357 (Givinostat)

相关生物数据

ITF2357 (Givinostat)

相关生物数据

ITF2357 (Givinostat)

ITF2357 (Givinostat) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

ITF2357 (Givinostat) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

化学性质

CAS号 732302-99-7 SDF Download SDF
别名 ITF-2357
化学名 (6-((diethylamino)methyl)naphthalen-2-yl)methyl (4-(hydroxycarbamoyl)phenyl)carbamate hydrochloride hydrate
SMILES CCN(CC)CC1=CC2=C(C=C(COC(NC3=CC=C(C(NO)=O)C=C3)=O)C=C2)C=C1.O.Cl
分子式 C24H27N3O4.HCl.H2O 分子量 475.97
溶解度 ≥23.8 mg/mL in DMSO, <2.61 mg/mL in EtOH, ≥2.9 mg/mL in H2O with ultrasonic and warming 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 Givinostat (ITF2357)是一种有效的HDAC抑制剂,作用于玉米HD2、HD1B和HD1A,非细胞实验中的IC50值分别为10 nM、7.5 nM和16 nM。
靶点 HDAC          
IC50 7.5 to 16 nM          

实验操作

细胞实验[1]:

细胞系

PBMC细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

超乙酰化:100 nM,24 h

应用

为了检测ITF2357对乙酰化的能力,静息PBMCs与该抑制剂在37℃孵育1小时后用LPS刺激。在3、6和24 h后制备细胞沉淀提取物,并检测总细胞提取物中的乙酰化赖氨酸。ITF2357存在时,LPS孵育3小时后出现明显的超乙酰化,并一直持续到24小时。

动物实验[1]:

动物模型

BALB/C和C57BL/6小鼠

剂量

BALB/C小鼠:5 mg/kg,C57BL/6小鼠:1或10 mg/kg;灌胃。

应用

小鼠通过灌胃的方式给予100μL的水或ITF2357(5 mg/kg),1小时后静脉注射200 ?g的ConA。24小时后采血用于评估血清ALT的水平。ITF2357减少了超过80%的ALT水平。1 mg/kg的ITF2357与10 mg/kg的剂量均可有效减少ConA肝炎。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Leoni F, Fossati G, Lewis E C, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Molecular Medicine, 2005, 11(1-12): 1.

研究更新

1. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis. Mol Med. 2011 May-Jun;17(5-6):391-6. doi: 10.2119/molmed.2011.00058. Epub 2011 Feb 11.
Abstract
In models of arthritis, ITF2357, an HDACi, reduced joint swelling and cell influx into the joint cavity, improved the chondrocyte metabolic function, decreased production of proinflammatory cytokines, ameliorates the severity scores and prevented bone destruction.
2. Class I and II histone deacetylase inhibition by ITF2357 reduces SLE pathogenesis in vivo. Clin Immunol. 2014 Mar;151(1):29-42. doi: 10.1016/j.clim.2014.01.002. Epub 2014 Jan 15.
Abstract
ITF2357, an inhibitor of class I and II HDAC, decreased renal disease, inflammatory cytokines and Th17 phenotype in NZB/W mice; while it increased the percentage of Tregs and Foxp3 acetylation.
3. The oral histone deacetylase inhibitor ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. Mol Med. 2011 May-Jun;17(5-6):369-77. doi: 10.2119/molmed.2010.00152. Epub 2010 Dec 22.
Abstract
ITF2357 is an HDAC inhibitor that inhibits production of nitrite, TNFα and IFNγ in peritoneal macrophages and splenocytes. ITF2357 normalized STZ-induced hyperglycemia in mice returning serum nitrite levels to nondiabetic values, improving islet and increasing glucose clearance; while it increased islet cell viability, enhanced insulin secretion, inhibited MIP-1α and MIP-2 release, reduced nitric oxide production and decreased apoptosis rates in vitro.
4. The histone deacetylase inhibitor ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro. J Acquir Immune Defic Syndr. 2010 May 1;54(1):1-9. doi: 10.1097/QAI.0b013e3181d3dca3.
Abstract
ITF2357, an HDAC inhibitor, has been evaluated for its efficacy on HIC-1 expression from latently infected cells and its effect on the surface expression of CXCR4 and CCR5.
5. Effects of the histone deacetylase inhibitor ITF2357 in autoinflammatory syndromes. Mol Med. 2011 May-Jun;17(5-6):363-8. doi: 10.2119/molmed.2011.00039. Epub 2011 Jan 25.
Abstract
ITF2357, an HDAC inhibitor, was used to treatment patients with autoflammatory syndrome, including 1 patient with TRAPS, 3 patients with HIDS and 4 patients with Schnitzler syndrome, in a pilot study where ITF2357-induced partial response was only observed in patients with Schnitzler syndrome.

产品描述

ITF2357(givinostat)是一种有效的I类和II类组蛋白去乙酰化酶(HDAC)抑制剂。在体外慢性骨髓增殖性肿瘤中,ITF2357也可以有效抑制JAKEV617F祖细胞的造血细胞集落形成。已有研究表明,ITF2357通过诱导p21,下调Bcl-2和Mcl-1蛋白,从而诱导多发性骨髓瘤(MM)细胞和急性骨髓性白血病(AML)细胞的凋亡。 在外周血单核细胞中,ITF2357抑制促炎细胞因子(比如IL-1、IL-6、肿瘤坏死因子(TNF)-α和干扰素(IFN)-γ)的产生。在间充质基质细胞中,ITF2357抑制IL-6和血管内皮生长因子(VEGF)的产生。

参考文献:
Katia Todoerti, Valentina Barbui, Olga Pedrini, Marta Linett, Gianluca Fossati, Paolo Mascagni, Alessandro Rambaldi, Antonino Neri, Martino Introna, Luigia Lombardi, and Josee Golay.  Pleiotropi anti-myeloma activity of ITF2357: inhibition of interleukin-6 receptor signaling and repression of miR-19a and miR-19b. Haematologica 2010; 95(2): 260-269