1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Stem Cell/Wnt Anti-infection PI3K/Akt/mTOR Apoptosis
  2. Glucose-6-Phosphate Isomerase (GPI) Casein Kinase Virus Protease Flavivirus PI3K Akt mTOR Apoptosis
  3. Rhodiolin

Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .

For research use only. We do not sell to patients.

Rhodiolin Chemical Structure

Rhodiolin Chemical Structure

CAS No. : 86831-53-0

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Description

Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral [1][2][3].

IC50 & Target[1]

CK1ε

 

PI3K

 

Akt

 

mTOR

 

Cellular Effect
Cell Line Type Value Description References
MDCK CC50
> 300 μM
Compound: 9
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
[PMID: 19729316]
In Vitro

Rhodiolin (0-40 μM, 24 h) induces cell cycle arrest at G1/S phase in PTC cells[1].
Rhodiolin (0-40 μM, 12-24 h) blocks glycolysis by down­regulating GPI expression and then inhibited the PI3K/Akt/mTOR signaling pathway which, in turn, inhibits the proliferation and induces the apoptosis of PTC cells[1].

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

Cell Cycle Analysis[1]

Cell Line: PTC cells
Concentration: 10, 20 and 40 μM
Incubation Time: 24 h
Result: Showed a dose-dependent reduction in S-phase cells.

Apoptosis Analysis[1]

Cell Line: PTC cells
Concentration: 10, 20 and 40 μM
Incubation Time: 12 h
Result: Observed A dose-dependent increase in the percentage of cells undergoing early apoptosis and late apoptosis.
Caused dose-dependent reduction in MMP.
Reduced the number of mitochondria in tumor cells significantly while increasing the intracellular oxidation level.

Western Blot Analysis[1]

Cell Line: PTC cells
Concentration: 10, 20 and 40 μM
Incubation Time: 24 h
Result: Decreased the expression of cyclin E, CDK4, and CDK2 .
Increased the expression of the expression of p21 and p27.
Reduced phosphorylation of the PI3K/Akt/mTOR signaling pathway significantly.
In Vivo

Rhodiolin (10-25 mg/kg, i,g., every two days for 10 days) significantly inhibits tumor growth in a human PTC xenograft model in BALB/c-nude mice[1].

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

Animal Model: MH-134 hepatoma xenograft model established in 6 weeks old female C57BL/6 mice[1]
Dosage: 10 and 25 mg/kg
Administration: Intragastric administration (i.g.), every two days for 10 days
Result: Reduced the tumor-cell density significantly.
Showed a dose-dependent reduction in the number of Ki-67-positive cells and GPI expression.
Induced significant apoptosis in tumor tissue.
No signs of hepatotoxicity were evident.
No morphological abnormalities or signs of inflammation were detected in the heart, liver, spleen, lungs, or kidneys of mice.
Molecular Weight

480.42

Formula

C25H20O10

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(O)C=C(O[C@H](C3=CC(OC)=C(O)C=C3)[C@@H](CO)O4)C4=C2OC(C5=CC=C(O)C=C5)=C1O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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    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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