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

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.

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cis-THSG

cis-THSG Chemical Structure

CAS No. : 928205-59-8

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Description

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

 

In Vitro

cis-THSG (100 μM; 30 min) exhibits weak inhibitory activity against human DNA topoisomerase II, with 46% inhibition at 100 μM, and no activity against DNA topoisomerase I[1].
cis-THSG shows no cytotoxicity against HT-29, MCF-7, and HepG2 cell lines[1].
Cis-THSG (30-100 μM; 8 h) suppresses Dexamethasone (HY-14648)/8-CTP-cAMP -induced PEPCK mRNA expression in HepG2 cells, with maximum inhibition (61.7% reduction) observed at 30 μM for 8 h[2].

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

In Vivo

Cis-THSG (0.01% in drinking water; ad libitum; daily; 12 weeks) exhibits potent anti-diabetic activity in HFD-induced male CF-1 diabetic mice, including significant reduction of hyperglycemia, hyperinsulinemia, and insulin resistance, and marked improvement of glucose intolerance[2].

MedChemExpress (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.
Molecular Weight

406.38

Formula

C20H22O9

CAS No.
SMILES

O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1OC2=C(/C=C\C3=CC=C(O)C=C3)C=C(O)C=C2O

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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cis-THSG
Cat. No.:
HY-N8250
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