同义名 :	-
	CAS号 :	28097-03-2
	货号 :	A595022
	分子式 :	C30H28N6O6S4
	纯度 :	99%+
	分子量 :	696.84
	MDL号 :	MFCD00133163
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -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 methylation plays a key role in establishing and maintaining stable gene expression patterns during cellular differentiation and embryonic development. Some histone methyltransferases (HMTs) are misregulated in tumors and methyltransferase-induced heterochromatin formation is related to neurodegenerative diseases. Histone methyltransferase SU(VAR)3-9 plays an critical role in establishing condensed heterochromatin by specifically methylating Lys9 of histone H3 and is conserved in most higher eukaryotes. Chaetocin, produced by Chaetomium sp, is a specific inhibitor of SU(VAR)3-9 with IC50 value of 0.8 uM, and also inhibits known Lys9-specific HMTs such as mouse G9a and Neurospora crassa DIM5 with IC50 values of 2.5 and 3 mM, respectively[3]. Mice, bearing mouse hepatoma cell line Hepa 1c1c-7 tumors, showed significant retarded tumor growth after intraperitoneally administrating with chaetocin at 0.25 mg/kg daily for 2 weeks. The hypoxic induction of HIF-1a was decreased in human hepatoma cell lines HepG2, Hep3B, and Huh7 when pretreated with chaetocin (0.05 and 0.1 uM) 1h prior to normoxic or hypoxic incubation for 8h[4]. Chaetocin at 10 - 30 nM inhibited IBMX-induced melanin synthesis in a dose-dependent manner which was relieved by suppression of ERK pathway[5].

细胞研究
细胞系	浓度	检测类型	检测时间	活性说明	数据源
A549 cells		Cytotoxicity assay		Cytotoxicity against human A549 cells, IC50=0.025 μM	20303767
Hep3b cells		Function assay		Inhibition of HIF-1alpha-mediated VEGF expression in human Hep3b cells by luciferase reporter gene assay, IC50=0.04 μM	22305612
HL60 cells	0.3 uM	Function assay	4 h	Induction of apoptosis in human HL60 cells assessed as nuclear fragmentation at 0.3 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis	20675131

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.44mL 0.29mL 0.14mL	7.18mL 1.44mL 0.72mL	14.35mL 2.87mL 1.44mL

参考文献

[1]Lee YM, Lim JH, et al. Antihepatoma activity of chaetocin due to deregulated splicing of hypoxia-inducible factor 1α pre-mRNA in mice and in vitro. Hepatology. 2011 Jan;53(1):171-80. [2]Greiner D, Bonaldi T, et al. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat Chem Biol. 2005 Aug;1(3):143-5. Epub 2005 Jul 17. [3]Greiner D, Bonaldi T, Eskeland R, Roemer E, Imhof A. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat Chem Biol. 2005 Aug;1(3):143-5. doi: 10.1038/nchembio721. Epub 2005 Jul 17. PMID: 16408017. [4]Lee YM, Lim JH, Yoon H, Chun YS, Park JW. Antihepatoma activity of chaetocin due to deregulated splicing of hypoxia-inducible factor 1α pre-mRNA in mice and in vitro. Hepatology. 2011 Jan;53(1):171-80. doi: 10.1002/hep.24010. Epub 2010 Dec 7. PMID: 21140472. [5]Bae JS, Han M, Yao C, Chung JH. Chaetocin inhibits IBMX-induced melanogenesis in B16F10 mouse melanoma cells through activation of ERK. Chem Biol Interact. 2016 Feb 5;245:66-71. doi: 10.1016/j.cbi.2015.12.021. Epub 2015 Dec 31. PMID: 26748310.