Chaetocin - CAS:28097-03-2

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Chaetocin (Synonyms:毛壳素)

目录号 : KM12667 CAS No. : 28097-03-2 纯度 : 98%

Data Sheet 产品使用指南

Chaetocin是组蛋白甲基转移酶(HMT) SU(VAR)3-9的特异性抑制剂，IC₅₀值为0.6 μM。Chaetocin也可抑制硫氧还蛋白还原酶(TrxR)，IC₅₀值为4 μM。

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1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC₅₀ of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC₅₀ of 4 μM.

体外研究

Chaetocin is initially isolated from the fermentation broth of chaetomium minutum and belongs to the class of 3-6 epidithio-diketopiperazines (ETPs). The IC₅₀ for SU(VAR)3-9 is 0.6 μM and acts as a competitive inhibitor for S-adenosylmethionine. Chaetocin inhibits the human ortholog of dSU(VAR)3-9 with a similar IC₅₀ value of 0.8 μM. It inhibits other known Lys9-specific HMTs such as mouse G9a and Neurospora crassa DIM5 with a higher IC₅₀ values of 2.5 and 3 mM, respectively. Chaetocin inhibits TrxR1-initiated turnover of the synthetic substrate DTNB in a cell-free assay in a dose-responsive manner with an IC₅₀ of about 4 μM.

体内研究

SL-2 Drosophila tissue cells are cultured in the presence or absence of the inhibitor. Chaetocin has a toxic effect on cells grown in culture. Toxicity is highly dependent on the initial cell density when chaetocin is added to the culture. The number of H3 molecules dimethylated at Lys9 (H3K9me2) is markedly reduced when cells are grown in medium containing 0.5 μM chaetocin after 5 d. Histones isolated from cells treated with 0.1 μM and for a shorter time also shows a drop in Lys9 methylation, but not as strongly as with the higher concentration.

分子式

C₃₀H₂₈N₆O₆S₄

分子量

696.84

CAS号

28097-03-2

中文名称

毛壳素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (17.94 mM; ultrasonic and warming and heat to 60°C)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: 2.08 mg/mL (2.98 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (2.98 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.08 mg/mL (2.98 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。