2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Topoisomerase PEPCK
  4. cis-THSG

cis-THSG 是口服有效的 DNA 拓扑异构酶 II (DNA topoisomerase II) 选择性抑制剂，对 DNA拓扑异构酶 I 无抑制活性。cis-THSG 可抑制磷酸烯醇式丙酮酸羧激酶 (PEPCK) 的转录表达。cis-THSG 可降低高脂饮食诱导的糖尿病雄性 CF-1 小鼠的血糖水平，改善其葡萄糖不耐受症状并缓解胰岛素抵抗。cis-THSG 可用于 2 型糖尿病的相关研究。

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cis-THSG

cis-THSG Chemical Structure

CAS No. : 928205-59-8

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cis-THSG 相关抗体

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Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus[1][2].

IC50 & Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

cis-THSG (100 μM; 30 min) 对人 DNA 拓扑异构酶 II 表现出弱抑制活性，在 100 μM 浓度下抑制率为 46%，且对 DNA 拓扑异构酶 I 无活性[1]。
cis-THSG 对 HT-29、MCF-7 和 HepG2 细胞系无细胞毒性[1]。
Cis-THSG (30-100 μM; 8 h) 可抑制 HepG2 细胞中 Dexamethasone (HY-14648)/8-CTP-cAMP 诱导的 PEPCK mRNA 表达，在 30 μM 作用 8 h 时抑制作用达到最强 (表达量降低 61.7%)[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

cis-THSG 相关抗体:
体内研究
(In Vivo)

Cis-THSG (饮水含 0.01%；自由摄取；每日；12 周) 在 HFD 诱导的雄性 CF-1 糖尿病小鼠中表现出强效的抗糖尿病活性，包括显著降低高血糖、高胰岛素血症与胰岛素抵抗，以及明显改善葡萄糖耐受不良[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CF-1 (male; HFD-induced type 2 diabetes mellitus)[2]
Dosage: 0.01% in drinking water
Administration: ad libitum; daily; 12 weeks
Result: Significantly decreased serum glucose levels in HFD-induced diabetic mice.
Significantly lowered elevated serum insulin levels and reduced calculated HOMA-IR by 102.7% compared to the trans-THSG treatment group.
Greatly suppressed the sharp rise in blood glucose at 30 minutes post-intraperitoneal glucose injection and reduced the sustained high blood glucose levels observed at 120 minutes, effectively ameliorating glucose intolerance.
分子量

406.38

Formula

C20H22O9
CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

cis-THSG 相关分类

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Keywords:

cis-THSG928205-59-8TopoisomerasePEPCKPhosphoenolpyruvate CarboxykinaseCF-1 miceHepG2human carcinoma cellstype 2 diabetes mellitusMCF-7phosphoenopyruvate carboxykinaseDNA topoisomerase IHT-29Polygonum multiflorum rootsDNA topoisomerase IIInhibitorinhibitorinhibit

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