Chaetocin
(Synonyms: 毛壳素) 目录号 : GC14936
据报道毛壳素是组蛋白甲基转移酶 (HMT)（例如 SUV39H1）的非特异性抑制剂，从而影响基因表达。
Cas No.:28097-03-2
Sample solution is provided at 25 µL, 10mM.
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Chaetocin was reported to be a nonspecific inhibitor of histone methyl transferase (HMT) such as SUV39H1, thereby affecting gene expression [1]. Chaetocin inhibited HMT SU(VAR)3-9 with an IC50 of 0.6 µM [2].
Chaetocin significantly reduces the proliferation, cloning potential, and migration ability of the glioblastoma cell line T98G [3]. Chaetocin abrogated the maintenance of stem cell characteristics and tumor growth of bladder cancer stem cells (BCSCs) by suppressing the KMT1A-GATA3-STAT3 circuit (inhibition ratio: 80.1%) [4]. Chaetocin inhibited ovarian cancer (OC) cell proliferation, induced G2/M phase cell cycle arrest, and induced apoptosis at the concentration of 2µM (24 hours) [5]. Chaetocin inhibited cell proliferation and reduced PI3K/AKT pathway and p-AKT in gastric cancer HGC-27 cell, at the concentration of 200µM (24 hours) [6].
Chaetocin inhibited tumor growth in HGC-27 cell injected Gastric cancer mice model, by 0.5 mg/kg/day every alternate day for 24 days [6]. Chaetocin inhibited tumor progression and reduced PCNA in U87MG cell injected glioma mice model, by 0.5 mg/kg/day every alternate day for 25 days [7].
References:
[1]. Cherblanc F L, Chapman K L, Brown R, et al. Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases[J]. Nature chemical biology, 2013, 9(3): 136-137.
[2]. Greiner D, Bonaldi T, Eskeland R, et al. Identification of a specific inhibitor of the histone methyltransferase SU (VAR) 3-9[J]. Nature chemical biology, 2005, 1(3): 143-145.
[3]. Sepsa A, Levidou G, Gargalionis A, et al. Emerging role of linker histone variant H1x as a biomarker with prognostic value in astrocytic gliomas. A multivariate analysis including trimethylation of H3K9 and H4K20[J]. PLoS One, 2015, 10(1): e0115101.
[4]. Yang Z, Wang H, Zhang N, et al. Chaetocin Abrogates the Self-Renewal of Bladder Cancer Stem Cells via the Suppression of the KMT1A-GATA3-STAT3 Circuit[J]. Frontiers in cell and developmental biology, 2020, 8: 424.
[5]. Li Z, Huang L, Wei L, et al. Chaetocin induces caspase?dependent apoptosis in ovarian cancer cells via the generation of reactive oxygen species[J]. Oncology Letters, 2019, 18(2): 1915-1921.
[6]. Wen C, Wang H, Wu X, et al. ROS-mediated inactivation of the PI3K/AKT pathway is involved in the antigastric cancer effects of thioredoxin reductase-1 inhibitor chaetocin[J]. Cell death & disease, 2019, 10(11): 1-16.
[7]. Dixit D, Ghildiyal R, Anto N P, et al. Chaetocin-induced ROS-mediated apoptosis involves ATM-YAP1 axis and JNK-dependent inhibition of glucose metabolism[J]. Cell death & disease, 2014, 5(5): e1212-e1212.
据报道毛壳素是组蛋白甲基转移酶 (HMT)（例如 SUV39H1）的非特异性抑制剂,从而影响基因表达[1]。 Chaetocin 抑制 HMT SU(VAR)3-9,IC50 为 0.6 µM [2]。
Chaetocin 显着降低 HMT SU(VAR)3-9 的增殖、克隆潜力和迁移能力胶质母细胞瘤细胞系 T98G [3]. Chaetocin 通过抑制 KMT1A-GATA3-STAT3 回路（抑制率:80.1%）,破坏了膀胱癌干细胞（BCSCs）干细胞特性的维持和肿瘤生长[4]。 Chaetocin 在浓度为 2µM（24 小时）[5] 时抑制卵巢癌 (OC) 细胞增殖,诱导 G2/M 期细胞周期停滞,并诱导细胞凋亡。 Chaetocin 在胃癌 HGC-27 细胞中抑制细胞增殖并降低 PI3K/AKT 通路和 p-AKT,浓度为 200µM（24 小时）[6]。
毛壳素在注射 HGC-27 细胞的胃癌小鼠模型中抑制肿瘤生长,每隔一天 0.5 mg/kg/天,持续 24 天[6]。 Chaetocin 在 U87MG 细胞注射神经胶质瘤小鼠模型中抑制肿瘤进展并减少 PCNA,每隔一天 0.5 mg/kg/天,持续 25 天[7]。
| Cell experiment [1]: | |
|
Cell lines |
SKOV-3, OVCAR-3, KGN and A2780 ovarian cancer (OC) cell line |
|
Preparation Method |
The OC cells were seeded in 96-well microplates (1×104 cells/well) and incubated at 37°C overnight. Following incubation with chaetocin (0.05, 0.1, 0.25, 0.5, 0.75, 1 and 2 µM) at 37°C for 24 h, |
|
Reaction Conditions |
0.05, 0.1, 0.25, 0.5, 0.75, 1 and 2 µM for 24 hours |
|
Applications |
Chaetocin significantly inhibited the viability of SKOV-3, OVCAR-3, KGN and A2780 cells in a dose-dependent manner, with half-maximal inhibitory concentrations of 0.30, 60.66, 81.86 and 100.60 nM, respectively. |
| Animal experiment [2]: | |
|
Animal models |
Female BALB/C nude mice |
|
Preparation Method |
Paired mice with equal tumor volume were divided into the chaetocin-treated group and the vehicle-treated group (n = 6 for each group), and then injected intraperitoneally (i.p.) daily with chaetocin (0.5 mg/kg) and the vehicle (DMSO), respectively. After 10 days of drug treatment, mice were sacrificed and the tumor were weighed. |
|
Dosage form |
Intraperitoneal injection, 0.5 mg/kg/day for 10 days |
|
Applications |
Significantly lower average tumor weight for chaetocin treatment group compared to control group |
|
References: [1]: Li Z, Huang L, Wei L, et al. Chaetocin induces caspase?dependent apoptosis in ovarian cancer cells via the generation of reactive oxygen species[J]. Oncology Letters, 2019, 18(2): 1915-1921. | |
| Cas No. | 28097-03-2 | SDF | |
| 别名 | 毛壳素 | ||
| 化学名 | (3S,3'S,6R,6'R,14R,14'R,16S,16'S)-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-2,2',3,3',6,6',7,7'-octahydro-1H,1'H-[14,14'-bi(3,11a-epidithiopyrazino[1',2':1,5]pyrrolo[2,3-b]indole)]-1,1',4,4'(15H,15'H)-tetraone | ||
| Canonical SMILES | O=C1[C@](CO)(SS2)N(C)C([C@]32N1[C@]4([H])[C@](C(C=CC=C5)=C5N4)([C@@]6(C(C=CC=C7)=C7N8)[C@@]8([H])N(C([C@](CO)(SS9)N%10C)=O)[C@]9(C6)C%10=O)C3)=O | ||
| 分子式 | C30H28N6O6S4 | 分子量 | 696.84 |
| 溶解度 | DMSO: 25 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.435 mL | 7.1752 mL | 14.3505 mL |
| 5 mM | 0.287 mL | 1.435 mL | 2.8701 mL |
| 10 mM | 0.1435 mL | 0.7175 mL | 1.435 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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