2. MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis Stem Cell/Wnt Epigenetics
  3. PARP p38 MAPK IAP Caspase Apoptosis JNK ERK
  4. Hellebrigenin

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.

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Hellebrigenin Chemical Structure

Hellebrigenin Chemical Structure

CAS No. : 465-90-7

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Based on 1 publication(s) in Google Scholar

Hellebrigenin Related Antibodies

Top Publications Citing Use of Products

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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cIAP cIAP-1 cIAP-2 XIAP

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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JNK1 JNK2 JNK3 JNK

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ERK ERK1 ERK2 ERK5 ERK8

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Description

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[1][2].

IC50 & Target

Caspase 3

 

Cellular Effect
Cell Line Type Value Description References
SK-MEL IC50
0.096 μM
Compound: 6
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
[PMID: 33882233]
In Vitro

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.

Hellebrigenin Related Antibodies

Cell Viability Assay[1]

Cell Line: SCC-1/SCC-47 (oral squamous cell carcinoma)
Concentration: 2-8 nM
Incubation Time: 24-72 h
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).
In Vivo

Hellebrigenin (6 mg/kg; intraperitoneal injection; 3 times/week; 4 weeks) significantly inhibits tumor growth in the mouse oral cancer SCC-1 cell xenograft model without affecting the mouse body weight[1].

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

Animal Model: C57BL/6 mice (male, 5-6 weeks old, 18-22 g), SCC-1 cell xenograft model[1]
Dosage: 6 mg/kg
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
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.
Molecular Weight

416.51

Formula

C24H32O6
CAS No.
Appearance

Solid

Color

White to off-white

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
Structure Classification
Initial Source

toad
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4009 mL 12.0045 mL 24.0090 mL
5 mM 0.4802 mL 2.4009 mL 4.8018 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.65%

SDS (252 KB)

COA (256 KB) HNMR (143 KB) CNMR (157 KB) RP-HPLC (280 KB) MS (153 KB)

Handling Instructions (2659 KB)
References

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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Hellebrigenin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Hellebrigenin465-90-7PARPp38 MAPKIAPCaspaseApoptosisJNKERKpoly ADP ribose polymerase c-Jun N-terminal kinaseExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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