Chaetocin is a specific inhibitor of thehistone methyltransferase(HMT) SU(VAR)3-9 with anIC₅₀of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with anIC₅₀of 4 μM.

IC50: 0.6 μM (HMT)^[1], 4 μM (TrxR)^[2]

Chaetocin is initially isolated from the fermentation broth ofchaetomium minutumand belongs to the class of 3-6 epidithio-diketopiperazines (ETPs). The IC₅₀for 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 IC₅₀value of 0.8 μM. It inhibits other known Lys9-specific HMTs such as mouse G9a andNeurospora crassaDIM5 with a higher IC₅₀values of 2.5 and 3 mM, respectively^[1]. Chaetocin inhibits TrxR1-initiated turnover of the synthetic substrate DTNB in a cell-free assay in a dose-responsive manner with an IC₅₀of about 4 μM^[2].

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^[1].

696.84

Solid

C₃₀H₂₈N₆O₆S₄

28097-03-2

毛壳素

• Alkaloids
• Alkaloid Dimers

Chaetomium species

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 26 mg/mL(37.31 mM)

*"≥" means soluble, but saturation unknown.

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 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。