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CAS No.: 28097-03-2

Chaetocin/毛壳素 Catalog No. CSN19229

Synonyms: 毛壳素

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU (VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DIM5 (Neurospora crassa)

IC50:3μM dSU (VAR)3-9

IC50:0.8μM EHMT2 mouse

IC50:2.5μM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 0.2 mg/kg^[3] (i.p.), 2 mg/kg^[4] (i.p.) Rat: 0.05 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.2 mg/kg^[3] (i.p.), 2 mg/kg^[4] (i.p.) Rat: 0.05 mg/kg^[5] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4350 mL
- 7.1752 mL
- 14.3505 mL
- 5 mM
- 0.2870 mL
- 1.4350 mL
- 2.8701 mL
- 10 mM
- 0.1435 mL
- 0.7175 mL
- 1.4350 mL

技术信息

CAS号

28097-03-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H28N6O6S4

运输

蓝冰

分子量

696.84

别名

毛壳素

溶解度

DMSO	350.0 mg/mL (502.3 mM)
Water	insoluble

动物实验配方

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靶点	Description	IC50
DIM5 (Neurospora crassa)		IC50:3μM
dSU (VAR)3-9		IC50:0.8μM
EHMT2 mouse		IC50:2.5μM

Chaetocin/毛壳素 Catalog No. CSN19229

靶点选择性

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