| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| Other Sizes |
| Targets |
STAT3 (signal transducer and activator of transcription 3); Corylin inhibits IL-6-induced STAT3 activation[1]
lncRNA GAS5 (long noncoding RNA growth arrest-specific 5) and EMT-related proteins (E-cadherin, N-cadherin, vimentin); Corylin regulates EMT via lncRNA GAS5[2] SIRT-1 (sirtuin 1) and β3-AR (β3-adrenergic receptor); Corylin activates SIRT-1 and β3-AR[3] |
|---|---|
| ln Vitro |
1. In IL-6-stimulated cells, Corylin (10 μM, 20 μM, 40 μM) dose-dependently inhibited STAT3 phosphorylation (Tyr705 and Ser727). Western blot analysis showed that 40 μM Corylin reduced p-STAT3 (Tyr705) levels by approximately 70% compared to the IL-6-only group, and also downregulated the expression of STAT3 target genes (Bcl-2, cyclin D1) [1]
2. In human hepatocellular carcinoma (HCC) cells (HepG2, Huh7), Corylin (5 μM, 10 μM, 20 μM) dose-dependently suppressed cell migration and invasion. Transwell assays revealed that 20 μM Corylin reduced HepG2 cell migration by ~65% and invasion by ~70% compared to the control group. Additionally, Corylin upregulated E-cadherin (epithelial marker) and downregulated N-cadherin/vimentin (mesenchymal markers) via increasing lncRNA GAS5 expression; PCR data showed that 20 μM Corylin increased GAS5 levels by ~2.5-fold [2] 3. In 3T3-L1 adipocytes, Corylin (1 μM, 5 μM, 10 μM) promoted adipose tissue browning: Oil Red O staining showed that 10 μM Corylin reduced lipid droplet size and increased the number of small lipid droplets. Western blot analysis demonstrated that Corylin (10 μM) upregulated SIRT-1, UCP1 (brown adipose marker), and β3-AR expression by ~1.8-fold, ~2.2-fold, and ~1.6-fold, respectively. In insulin-resistant 3T3-L1 adipocytes, 10 μM Corylin improved insulin sensitivity by increasing Akt phosphorylation (Ser473) by ~1.7-fold [3] |
| ln Vivo |
1. In nude mouse models of HCC xenografts (HepG2 cells injected subcutaneously), Corylin was administered intragastrically at 20 mg/kg and 40 mg/kg once daily for 21 days. At the end of treatment, the 40 mg/kg group showed a ~55% reduction in tumor volume and a ~50% reduction in tumor weight compared to the vehicle group. Immunohistochemistry of tumor tissues revealed that Corylin (40 mg/kg) upregulated E-cadherin and lncRNA GAS5, and downregulated N-cadherin and vimentin [2]
2. In high-fat diet (HFD)-induced obese C57BL/6 mice, Corylin was administered intragastrically at 10 mg/kg and 20 mg/kg once daily for 8 weeks. The 20 mg/kg group showed a ~25% reduction in body weight, ~30% reduction in epididymal white adipose tissue (eWAT) weight, and ~40% reduction in fasting blood glucose compared to the HFD group. Additionally, Corylin (20 mg/kg) increased UCP1 expression in eWAT (by ~2.0-fold) and improved insulin resistance (HOMA-IR index reduced by ~35%) via activating SIRT-1 and β3-AR [3] |
| Enzyme Assay |
SIRT-1 activity assay: Recombinant SIRT-1 enzyme was incubated with a fluorogenic substrate (acetyl-peptide) and different concentrations of Corylin (0.1 μM, 1 μM, 5 μM, 10 μM) in reaction buffer at 37°C for 1 hour. After adding the deacetylation detection reagent, the fluorescence intensity (excitation: 360 nm, emission: 460 nm) was measured. The results showed that Corylin dose-dependently increased SIRT-1 activity, with 10 μM Corylin enhancing activity by ~1.5-fold compared to the control [3]
|
| Cell Assay |
1. IL-6-induced STAT3 activation assay in cells: Cells were seeded in 6-well plates and cultured to 70% confluence. After serum starvation for 12 hours, cells were pretreated with Corylin (10 μM, 20 μM, 40 μM) for 2 hours, then stimulated with IL-6 (10 ng/mL) for 30 minutes. Cells were lysed, and the levels of p-STAT3 (Tyr705/Ser727), total STAT3, and target genes (Bcl-2, cyclin D1) were detected by Western blot [1]
2. HCC cell migration and invasion assay: HepG2/Huh7 cells were seeded in 6-well plates and treated with Corylin (5 μM, 10 μM, 20 μM) for 48 hours. For migration assays, cells were trypsinized, resuspended in serum-free medium, and added to the upper chamber of Transwell inserts; the lower chamber contained medium with 10% FBS. After 24 hours, non-migrated cells on the upper surface were removed, and migrated cells were stained and counted. For invasion assays, Transwell inserts were pre-coated with Matrigel, and the same steps as migration assays were followed [2] 3. 3T3-L1 adipocyte browning and insulin sensitivity assay: 3T3-L1 preadipocytes were induced to differentiate into adipocytes, then treated with Corylin (1 μM, 5 μM, 10 μM) for 7 days. Oil Red O staining was used to observe lipid droplet morphology. For insulin sensitivity detection, differentiated adipocytes were treated with Corylin for 24 hours, then stimulated with insulin (100 nM) for 15 minutes, and Akt phosphorylation (Ser473) was detected by Western blot [3] |
| Animal Protocol |
1. HCC xenograft nude mouse model: Male BALB/c nude mice (4-6 weeks old) were subcutaneously injected with 5×10⁶ HepG2 cells into the right flank. When tumors reached ~100 mm³, mice were randomly divided into 3 groups (n=6/group): vehicle group (0.5% CMC-Na), Corylin 20 mg/kg group, and Corylin 40 mg/kg group. Corylin was dissolved in 0.5% CMC-Na and administered intragastrically once daily for 21 days. Tumor volume was measured every 3 days, and mice were euthanized at the end of treatment to collect tumors for weight measurement and immunohistochemistry [2]
2. HFD-induced obese mouse model: Male C57BL/6 mice (6 weeks old) were fed a HFD (60% fat) for 8 weeks to induce obesity, then randomly divided into 3 groups (n=8/group): HFD group (vehicle), Corylin 10 mg/kg group, and Corylin 20 mg/kg group. Corylin was dissolved in 0.5% CMC-Na and administered intragastrically once daily for another 8 weeks. Body weight was measured weekly; at the end of the experiment, fasting blood glucose was detected, and eWAT was collected for Western blot (UCP1, SIRT-1, β3-AR) analysis [3] |
| References |
|
| Additional Infomation |
Corylene is an isoflavone compound.
Corylene has been reported to exist in Ficus mucuso, Erythrina addisoniae, and other organisms with relevant data. Corylene is a phenolic compound isolated from the seeds of Psoralea corylifolia, a traditional Chinese medicine [1]. Corylene's inhibitory effect on STAT3 activation is independent of IL-6 receptor expression, as Western blot results showed no significant change in IL-6R levels after corylene treatment [1]. In hepatocellular carcinoma (HCC) cells, corylene-mediated upregulation of lncRNA GAS5 is crucial for EMT inhibition: GAS5 siRNA transfection reversed corylene-induced upregulation of E-cadherin and downregulation of N-cadherin/vimentin [2]. Corylin-induced adipose tissue browning is dependent on SIRT-1 and β3-AR: treatment with SIRT-1 inhibitors (EX527) or β3-AR antagonists (SR59230A) can block Corylin-mediated increase in UCP1 expression and improvement in insulin resistance [3] |
| Molecular Formula |
C20H16O4
|
|---|---|
| Molecular Weight |
320.3386
|
| Exact Mass |
320.104
|
| CAS # |
53947-92-5
|
| PubChem CID |
5316097
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
527.4±50.0 °C at 760 mmHg
|
| Flash Point |
193.1±23.6 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.637
|
| LogP |
4.45
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
24
|
| Complexity |
576
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PWAACAMQKVIVPZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H16O4/c1-20(2)8-7-13-9-12(3-6-17(13)24-20)16-11-23-18-10-14(21)4-5-15(18)19(16)22/h3-11,21H,1-2H3
|
| Chemical Name |
3-(2,2-dimethylchromen-6-yl)-7-hydroxychromen-4-one
|
| Synonyms |
Corylin
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~312.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1217 mL | 15.6084 mL | 31.2168 mL | |
| 5 mM | 0.6243 mL | 3.1217 mL | 6.2434 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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