产品说明书

	同义名 :	HDAC6 Inhibitor;Histone Deacetylase 6;MPI5a
	CAS号 :	1259296-46-2
	货号 :	A698765
	分子式 :	C16H17N3O3
	纯度 :	97%
	分子量 :	299.32
	MDL号 :	MFCD29770783
	存储条件：	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states[1]. HDAC modulates cell proliferation and angiogenesis and plays an essential role in cell growth. Research shows that up-regulated HDACs are present in many cancer types and synthetic or natural HDAC inhibitors have been used to silence overregulated HDACs. Inhibiting HDACs may cause arrest of cell proliferation, angiogenesis reduction and cell apoptosis[2].In plasma from animals exposed to [HDAC inhibitor + anti-PD-1], but not [HDAC inhibitor + anti-CTLA4], the levels of CCL2, CCL5, CXCL9 and CXCL2 were increased. The cytokine data from HDAC inhibitor plus anti-PD-1 exposed tumors correlated with increased activated T cell, M1 macrophage, neutrophil and NK cell infiltration[3].Treatment with HDAC inhibitors results in the hyperacetylation of chaperones including heat shock protein (hsp)90, hsp70, hsp40, and the ER-resident hsp70 homolog, glucose-regulated protein 78 (GRP78), which affects their function. HDAC inhibitor-mediated deregulation of chaperone function, in turn, deregulates protein homeostasis and induces protein misfolding and proteotoxic stress. In the context of tumors which are particularly dependent on functional chaperones for maintaining protein homeostasis, HDAC inhibitors tip the balance toward lethal proteotoxic and ER stress[4].HDAC6 Inhibitor(MPI_5a) is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM)[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.34mL 0.67mL 0.33mL	16.70mL 3.34mL 1.67mL	33.41mL 6.68mL 3.34mL

参考文献

[1] Somy Yoon, Gwang Hyeon Eom. HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases. Chonnam Med J. 2016 Jan;52(1):1-11. [2]I-Chung Chen,et al. Recent Update of HDAC Inhibitors in Lymphoma. Front Cell Dev Biol. 2020 Sep 3;8:576391. [3]Laurence Booth,et al. HDAC inhibitors enhance the immunotherapy response of melanoma cells. Oncotarget.2017 May 17;8(47):83155-83170. [4]Rekha Rao,et al. HDAC inhibitors and chaperone function. Adv Cancer Res. 2012;116:239-62. [5]Blackburn C, et al. Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform. J Med Chem. 2013 Sep 26;56(18):7201-11.