1. MAPK/ERK Pathway Apoptosis Autophagy
  2. JNK Apoptosis Autophagy
  3. Juglanin

Juglanin, a occurring flavonoid that can be isolated from crude Polygonum aviculare, is a JNK acticator, with anti-inflammatory, anti-oxidant and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells.

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Juglanin Chemical Structure

Juglanin Chemical Structure

CAS No. : 5041-67-8

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1 mg USD 140 In-stock
5 mg USD 350 In-stock
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Based on 5 publication(s) in Google Scholar

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Description

Juglanin, a occurring flavonoid that can be isolated from crude Polygonum aviculare, is a JNK acticator, with anti-inflammatory, anti-oxidant and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells[1][2].

IC50 & Target[1]

JNK

 

In Vitro

Juglanin (0-40 μM, 24-48 h) inhibits the proliferation of breast cancer cell in a dose- and time-dependent manner and presents less cytotoxic against the normal cells[1].
Juglanin (0-10 μM, 24 h) induces the G2/M phase arrest and Caspase-dependent apoptosis in MCF-7/SKBR3 cells[1].
Juglanin (10 μM, 24 h) promotes ROS generation and enhances JNK activation in MCF-7/SKBR3 cells[1].
Juglanin (40-160 μM, 24 h) inhibits inflammation and attenuates neuroinflammation in Lipopolysaccharides (LPS, HY-D1056)-treated AST cells[2].
Juglanin (40 μM, 24 h) inhibits Sting expression in TGF-β1-incubated MRC-5 cells[3].

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

Cell Viability Assay[3]

Cell Line: MCR-5 cell
Concentration: 0-40 μM
Incubation Time: 0-72 h
Result: Reduced the cell viability of MCR-5 after 24 h exposure at 160 μM.
Reduced the cell viability of MCR-5 after 72 h exposure at 40 μM.

Western Blot Analysis[1]

Cell Line: MCF-7, SKBR3
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased the expressions of phosphorylated Chk2, Chk2, phosphorylated Cdc25C, phosphorylated Cdc2, p27, cyclin D, Bad, Bax and decreased the levels of Cdc25C, Cdc2, Bcl-2.
Activated caspases and led to Casapse-9, Casapse-8 and Caspase-3 cleavage.
Increased the level of JNK phosphorylation.

Western Blot Analysis[2]

Cell Line: Lipopolysaccharides (LPS, HY-D1056)-treated AST cells
Concentration: 40-160 μM
Incubation Time: 24 h
Result: Decreased the expression of TLR4, MyD88, CD14, p-IKKα, p-IκBα, p-NF-κB, GFAP, BDNF, Aβ and p-Tau induced by LPS (HY-D1056).
Increased the level of SYP, PSD-25 and SNAP-25.
In Vivo

Juglanin (10-20 mg/kg, i.p., daily, 7 days) inhibits growth of human breast cancer xenograft in a tumor-transplanted mouse model[1].
Juglanin (10-30 mg/kg, i.p., 5 times weekly) ameliorates neuroinflammation-related memory impairment and neurodegeneration through impeding TLR4/NF-κB in C57BL6 male mice[2].
Juglanin (80 mg/kg, i.g., daily, 21 days) protects against bleomycin (BLM, HY-108345)-induced lung injury by inhibiting fibrosis in C57BL/6 male mice[3].

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

Animal Model: Tumor-transplanted mouse model [1]
Dosage: 10-20 mg/kg
Administration: Intraperitoneal injection (i.p.), daily, 7 days
Result: Increased levels of cleaved Caspase-9 and Caspase-3, LC3BI, LC3BII and phosphorylated JNK.
Increased dead cells and apoptosis proportion in juglanin-treated tumor tissues.
Increase in mean areas that stained positively cleaved Caspase-3 in juglanin-treated tumor tissues.
Animal Model: C57BL6 male mice[2]
Dosage: 10-30 mg/kg
Administration: Intraperitoneal injection (i.p.), 5 times weekly
Result: Increased number of platform crossings and expanded time in target quadrant.
Decreased the expression level of α-synuclein, pro-inflammatory cytokines (IL-1β, TNF-α, IL-18 and COX-2), TLR-4, MyD88, CD14, Aβ, phosphorylation of Tau, Ibal and neurotrophic factor (BDNF).
Reversed LPS-triggered effect on synaptic markers, up-regulating the expression of SYP, PSD-95 and SNAP-25.
Restored TH levels in the hippocampus of mice in a dose-dependent manner.
Decreased p-IKKα, p-IκBα and p-NF-κB levels combinated with LPS.
Decreased the GFAP-positive cells.
Animal Model: C57BL/6 male mice[3]
Dosage: 80 mg/kg
Administration: i.g., daily, 1-21 days
Result: Improved the survial rate of the BLM (HY-108345)-treated mice.
Decreased the expression of BALF, CXCL1, IL-6, TNF-α, MPO activity, TGF-β1, and its down-streaming proteins (fibronectin/MMP-9/α-SMA/collagen I) Reduced the number of total cells, neutrophils and macrophages in BALF.
Molecular Weight

418.35

Formula

C20H18O10

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1C(O[C@@H]2O[C@@H](CO)[C@H](O)[C@H]2O)=C(C3=CC=C(O)C=C3)OC4=CC(O)=CC(O)=C41

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (239.03 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 2.3903 mL 11.9517 mL 23.9034 mL
5 mM 0.4781 mL 2.3903 mL 4.7807 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). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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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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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)

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: 99.90%

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). 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 2.3903 mL 11.9517 mL 23.9034 mL 59.7586 mL
5 mM 0.4781 mL 2.3903 mL 4.7807 mL 11.9517 mL
10 mM 0.2390 mL 1.1952 mL 2.3903 mL 5.9759 mL
15 mM 0.1594 mL 0.7968 mL 1.5936 mL 3.9839 mL
20 mM 0.1195 mL 0.5976 mL 1.1952 mL 2.9879 mL
25 mM 0.0956 mL 0.4781 mL 0.9561 mL 2.3903 mL
30 mM 0.0797 mL 0.3984 mL 0.7968 mL 1.9920 mL
40 mM 0.0598 mL 0.2988 mL 0.5976 mL 1.4940 mL
50 mM 0.0478 mL 0.2390 mL 0.4781 mL 1.1952 mL
60 mM 0.0398 mL 0.1992 mL 0.3984 mL 0.9960 mL
80 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7470 mL
100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5976 mL
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  • 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.

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