Glucoerucin
Glucoerucin potassium is an orally active PTP1B non-competitive allosteric inhibitor (IC50 = 6.07 μM) and H2S donor that can be isolated and extracted from Eruca sativa. Glucoerucin potassium upregulates the Nrf2 pathway and promotes irisin/UCP1-mediated adipose tissue browning through conversion to erucin or acting as a sustained-release H2S donor, thereby regulating metabolic and cardiovascular functions. Glucoerucin potassium also exerts anticancer effects by upregulating epoxide hydrolase and through non-competitive allosteric inhibition of PTP1B. Glucoerucin potassium can be used in research on obesity, cancer, type 2 diabetes, and cardiovascular and cerebrovascular diseases.
For research use only. We do not sell to patients.
- CAS No.: 21973-56-8
- Formula: C12H23NO9S3
- Molecular Weight:421.51
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Endogenous Metabolite Isoforms
More
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
2.5 μM
|
Antiproliferative activity against human erythroleukemic K562 cells assessed as inhibition of cell growth after 6 days by electronic counting with a Coulter Counter using in situ myrosinase hydrolysis of glucoerucin.
Antiproliferative activity against human erythroleukemic K562 cells assessed as inhibition of cell growth after 6 days by electronic counting with a Coulter Counter using in situ myrosinase hydrolysis of glucoerucin.
|
jf9503523 |
| K562 | IC50 |
3.0 μM
|
Antiproliferative activity against human erythroleukemic K562 cells assessed as inhibition of cell growth after 6 days by electronic counting with a Coulter Counter using pre-mix myrosinase hydrolysis of glucoerucin.
Antiproliferative activity against human erythroleukemic K562 cells assessed as inhibition of cell growth after 6 days by electronic counting with a Coulter Counter using pre-mix myrosinase hydrolysis of glucoerucin.
|
jf9503523 |
In Vitro
Glucoerucin potassium (0.1-500 µM; 6 days) shows almost no inhibitory activity against the proliferation of human erythroleukemia K562 cells[4].
Glucoerucin potassium (1.5 g; 37 °C) is completely hydrolyzed by myrosinase from Sinapis alba to give erucin in 82% yield[8].
Glucoerucin potassium (1 mM; 6 h) is oxidized by a 4-fold excess of H2O2 in water at room temperature to glucoraphanin with a conversion rate of 97%[8].
Glucoerucin potassium (0.1-200 µM; 30 min) inhibits recombinant human PTP1B non-competitively in a cell-free pNPP assay, with an IC50 of 6.07 µM and a Ki of 6.29 µM[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:cells from rat lung sections
-
Concentration:1, 2.5, 10, 25 µM
-
Incubation Time:24 h
-
Result:Significantly upregulated the protein expression of CYP1A1 and CYP1B1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Balb/c mice (high-fat diet (HFD)-induced mouse obesity model)[6]
-
Dosage:10 mg/kg
-
Administration:p.o.; once daily; 10 weeks
-
Result:Improved glycemic and lipid metabolism, and significantly reduced triglycerides.
Decreased the deposition of visceral white adipose tissue (vWAT) and the volume of white adipocytes.
Alleviated inflammation (reduced IL-6) and oxidative stress (restored Nrf2 levels) in vWAT.
Increased the expression of PGC-1α and FNDC5 in skeletal muscle, elevated blood irisin levels, and up-regulated UCP1 expression in vWAT, promoting browning and thermogenesis.
Chemical Information
-
CAS No. 21973-56-8
-
Molecular Weight 421.51
-
Formula C12H23NO9S3
-
SMILES
CSCCCC/C(S[C@@H]1O[C@@H]([C@H]([C@@H]([C@H]1O)O)O)CO)=N/OS(=O)(O)=O
-
Structure Classification
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)