Hellebrigenin
Based on 1 Customer Validation
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 465-90-7
- Formula: C24H32O6
- Molecular Weight:416.51
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Caspase Isoforms
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Biological Activity
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Caspase 3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL | IC50 |
0.096 μM
Compound: 6
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Cytotoxicity against human SK-MEL cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human SK-MEL cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
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[PMID: 33882233] |
Cell viability: Hellebrigenin (2-8 nM; 24-72 h) inhibits the cell viability of oral cancer SCC-1/47 cells and liver cancer HepG2 cells in a dose/time dependent manner[1][2].
Apoptosis: Hellebrigenin (2-8 nM; 24 h) induces oral cancer cells, activated Caspase-3/8/9 and PARP cleavage, accompanied by Bax/Bak upregulation and Bcl-2/Bcl-xL, Cyclin A2/B1, and CDK4/6 downregulation[1].
Hellebrigenin triggeres a decrease in mitochondrial membrane potential and Caspase cascade reaction in HepG2 cells[2].
WB verification: Hellebrigenin (8 nM; 24 h) down-regulates the levels of p-ERK/p38/p-JNK and XIAP expression in oral cancer cells, and inhibits Akt phosphorylation in HepG2 cells[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCC-1/SCC-47 (oral squamous cell carcinoma)
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Concentration:2-8 nM
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Incubation Time:24-72 h
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Result:Dose- and time-dependent reduction in viability (IC50=0.1-0.4 nM at 72 h) and colony formation (8 nM: 50% reduction vs. control).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male, 5-6 weeks old, 18-22 g), SCC-1 cell xenograft model[1]
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Dosage:6 mg/kg
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Administration:Oral gavage, 3 times/week, starting 7 days after subcutaneous injection of SCC-1 cells (2×106 cells/mouse) into the right flank, continued until sacrifice
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Result:Significantly reduced tumor volume (calculated as 0.5 × length × width2) by 50% and tumor weight by 40% compared to the vehicle control group. Tumor volume in the treatment group reached 400 mm3 at the end of the experiment, while the control group showed a progressive increase to 800 mm3.
Chemical Information
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CAS No. 465-90-7
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Appearance Solid
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Molecular Weight 416.51
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Formula C24H32O6
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Color White to off-white
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SMILES
O=C[C@@]12[C@]3([H])[C@](CC[C@@]1(C[C@@H](O)CC2)O)([H])[C@@]4([C@@](C)([C@@H](C(C=C5)=COC5=O)CC4)CC3)O
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Structure Classification
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Initial Source
toad
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 50 mg/mL (120.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.00 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.00 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hsieh MJ, et al. Hellebrigenin induces oral cancer cell apoptosis by modulating MAPK signalling and XIAP expression. J Cell Mol Med. 2024 Jan;28(2):e18071. [Content Brief]
[2]. Deng LJ, et al. Hellebrigenin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Chem Biol Interact. 2014 Aug 5;219:184-94. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4009 mL | 12.0045 mL | 24.0090 mL | 60.0226 mL |
| 5 mM | 0.4802 mL | 2.4009 mL | 4.8018 mL | 12.0045 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4009 mL | 6.0023 mL | |
| 15 mM | 0.1601 mL | 0.8003 mL | 1.6006 mL | 4.0015 mL | |
| 20 mM | 0.1200 mL | 0.6002 mL | 1.2005 mL | 3.0011 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9604 mL | 2.4009 mL | |
| 30 mM | 0.0800 mL | 0.4002 mL | 0.8003 mL | 2.0008 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6002 mL | 1.5006 mL | |
| 50 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0004 mL | |
| 80 mM | 0.0300 mL | 0.1501 mL | 0.3001 mL | 0.7503 mL | |
| 100 mM | 0.0240 mL | 0.1200 mL | 0.2401 mL | 0.6002 mL |
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