| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
- Caspase family (caspase-3, caspase-8, caspase-9) [1]
- Apoptosis-related proteins (Bax, Bcl-2) [1] - Human leukemia cells (HL-60: IC50 = 12.5 ± 1.3 μM; U937: IC50 = 15.7 ± 1.5 μM) [1] |
|---|---|
| ln Vitro |
- Gardenin B exhibited dose-dependent cytotoxicity against human leukemia cells. For HL-60 cells, IC50 was 12.5 ± 1.3 μM; for U937 cells, IC50 was 15.7 ± 1.5 μM (48-hour incubation) [1]
- It induced apoptosis in leukemia cells: 20 μM Gardenin B increased the apoptotic rate of HL-60 cells by 58±4% and U937 cells by 52±3% (Annexin V-FITC/PI staining) [1] - The compound activated multiple caspases: 20 μM increased cleaved caspase-3, -8, -9 protein levels by 3.2±0.3, 2.8±0.2, and 2.5±0.2-fold, respectively, in HL-60 cells [1] - It altered the Bax/Bcl-2 ratio: 20 μM elevated the Bax/Bcl-2 ratio by 3.8±0.3-fold in HL-60 cells, promoting mitochondrial apoptotic pathway activation [1] - It did not induce reactive oxygen species (ROS) generation: Even at 30 μM, ROS levels in HL-60 cells showed no significant difference from the control group [1] - It showed low cytotoxicity to normal human peripheral blood mononuclear cells (PBMCs): Cell viability remained above 80% at concentrations up to 30 μM [1] |
| Enzyme Assay |
- Caspase activity assay: HL-60 cells were treated with Gardenin B (10, 20, 30 μM) for 24 hours. Cell lysates were incubated with caspase-3/-8/-9 specific fluorogenic substrates, and fluorescence intensity was measured at excitation/emission wavelengths of 400/505 nm to quantify caspase activity [1]
- ROS detection assay: Leukemia cells were loaded with a ROS-specific fluorescent probe after treatment with Gardenin B (10–30 μM) for 24 hours. Fluorescence at 488/525 nm was detected to confirm no ROS overproduction [1] |
| Cell Assay |
- Cell viability assay: HL-60 and U937 cells were seeded in 96-well plates (5×10³ cells/well) and incubated overnight. Gardenin B (5–30 μM) was added, and cells were cultured for 48 hours. MTT reagent was added, and absorbance was measured at 570 nm to calculate IC50 values [1]
- Apoptosis detection assay: Leukemia cells were treated with Gardenin B (10, 20 μM) for 48 hours, stained with Annexin V-FITC and PI, and analyzed by flow cytometry to determine apoptotic rates [1] - Protein expression assay: Cells were treated with the compound (10, 20 μM) for 24 hours. Total protein was extracted for Western blot analysis of cleaved caspase-3/-8/-9, Bax, and Bcl-2 [1] - Normal cell cytotoxicity assay: Human PBMCs were treated with Gardenin B (10–30 μM) for 48 hours, and cell viability was measured by MTT assay [1] |
| Toxicity/Toxicokinetics |
Selective toxicity: It has strong cytotoxicity to leukemia cells (IC50 12.5–15.7 μM), but low toxicity to normal peripheral blood mononuclear cells (PBMCs) (cell viability >80% at 30 μM) [1]
- No oxidative stress induction: It does not produce reactive oxygen species (ROS) in leukemia cells, avoiding non-specific oxidative damage [1] |
| References | |
| Additional Infomation |
Gardenin B is a tetramethoxyflavonoid, a derivative of hesperidin in which the methoxy group at the 5-position is replaced by a hydroxyl group. It is a plant metabolite. It is both a tetramethoxyflavonoid and a monohydroxyflavonoid. Its function is related to that of hesperidin. Gardenin B has been reported to be found in citrus (Citrus tankan), citrus (Citrus reticulata), and other organisms with relevant data.
- Citrus fulvic acid B is a natural flavonoid compound isolated from plants[1] - Its anti-leukemia mechanism involves activation of caspase-dependent apoptosis pathways (endogenous and exogenous pathways), specifically by upregulating Bax, downregulating Bcl-2, and cleaving caspase-3/-8/-9[1] - The cell death it induces is independent of the production of reactive oxygen species (ROS), which distinguishes it from ROS-mediated anticancer drugs[1] - Due to its selective toxicity to leukemia cells, it shows potential as a candidate drug for targeted anti-leukemia[1] |
| Molecular Formula |
C19H18O7
|
|---|---|
| Molecular Weight |
358.3420
|
| Exact Mass |
358.105
|
| CAS # |
2798-20-1
|
| PubChem CID |
96539
|
| Appearance |
Light yellow to green yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
582.0±50.0 °C at 760 mmHg
|
| Melting Point |
180-181ºC
|
| Flash Point |
210.8±23.6 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.593
|
| LogP |
2.27
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
526
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LXEVSYZNYDZSOB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H18O7/c1-22-11-7-5-10(6-8-11)13-9-12(20)14-15(21)17(23-2)19(25-4)18(24-3)16(14)26-13/h5-9,21H,1-4H3
|
| Chemical Name |
5-hydroxy-6,7,8-trimethoxy-2-(4-methoxyphenyl)chromen-4-one
|
| 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 : ~10 mg/mL (~27.91 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.98 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 1.67 mg/mL (4.66 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7906 mL | 13.9532 mL | 27.9065 mL | |
| 5 mM | 0.5581 mL | 2.7906 mL | 5.5813 mL | |
| 10 mM | 0.2791 mL | 1.3953 mL | 2.7906 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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