2. Autophagy Apoptosis PI3K/Akt/mTOR Epigenetics Stem Cell/Wnt JAK/STAT Signaling Immunology/Inflammation TGF-beta/Smad MAPK/ERK Pathway NF-κB Metabolic Enzyme/Protease
  3. Autophagy Apoptosis AMPK mTOR STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP
  4. Phellodendrine chloride

Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

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Phellodendrine chloride

Phellodendrine chloride Chemical Structure

CAS No. : 104112-82-5

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Based on 1 publication(s) in Google Scholar

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Phellodendrine chloride Related Antibodies

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1 Publications Citing Use of MCE Phellodendrine chloride

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mTOR mTORC1 mTORC2

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STAT3 STAT5 STAT6 STAT1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway[1][2][3][4][5][6].

IC50 & Target[3][4][7]

IL-6

 

STAT3

 

MMP-3

 

IL-1β

 

IL-4

 

In Vitro

Phellodendrine chloride (0.6-80 μM, 24 h-14 d) significantly inhibits the proliferation and colony formation ability of KRAS-mutated PANC-1 and MiaPaCa-2 cells and its driven macropinocytosis, while showing no obvious toxicity to KRAS wild-type BxPC-3 cells and normal pancreatic cells HPDE6-c7[1].
Phellodendrine (10-40 μM, 12-24 h) diminishes the albumin (Alb) driven intracellular glutamine level, induces reactive oxygen species generation and causes mitochondrial membrane potential (MMP) depolarization in PANC-1 cells[1].
Phellodendrine chloride (5-40 μM, 0-48 h) induces apoptosis cell death in PANC-1 cells through caspase-dependent mitochondrial intrinsic pathway[1].
Phellodendrine (5-20 μM) chloride activates the p-AMPK/mTOR signalling pathway, as well as autophagy in Caco-2 cells stimulated by H2O2[2].
Phellodendrine chloride (5 μM) attenuates Monosodium urate (MSU) (HY-B2130A)-induced MMP3 production and proteoglycan degradation by inhibiting IL-6/STAT3 pathway in rabbit primary chondrocytes and C28/I2 cells (human normal chondrocytes)[3].
Phellodendrine (0-50 μM) chloride reduces the mRNA expression of MRGPRB3 and responsiveness of MRGPRX2 by altering its structure, is able to decrease Ca2+ levels, phosphorylation levels of CaMK, PLCβ1, PKC, ERK, JNK, p38, and p65, and inhibits the degradation of IκB-α in RBL-2H3 cells[4].
Phellodendrine (25-200 μg/mL, 37 h) chloride increases the survival rate of zebrafish embryos and restores the abnormal heart rate levels[5].
Phellodendrine (50-200 μg/mL, 13 h) chloride reduces the ROS level in zebrafish embryos and inhibits lipid peroxidation[5].
Phellodendrine (100 μg/mL) chloride reverses the expression of AKT and NF-κB3, IKK, COX-2 which were abnormally changed by AAPH (HY-Y0525)-induced oxidative stress in zebrafish embryos[5].
Phellodendrine (2.5-160 μg/mL, 24-48 h) chloride has an anti-MDD effect by regulating the mRNA levels of CHRM1, HTR1A and key targets of the PI3K/Akt signalling pathway (PI3K, Akt, mTOR) in PC12 cells[6].

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

Phellodendrine chloride Related Antibodies

Apoptosis Analysis[1]

Cell Line: PANC-1 cells
Concentration: 10, 20 and 40 μM
Incubation Time: 48 h
Result: Showed a higher apoptosis cells ratio both in early and late apoptosis.
Revealed a marked increase in the number of cells showing nuclear condensation and fragmentation.

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 0, 6, 12, 24 h
Result: Induced the expressions of apoptotic proteins (cleaved caspase-3, 7, 9, PARP and Bax) and reduced the levels of Bcl-2 in time and dose dependent manner.

Cell Viability Assay[7]

Cell Line: PC12 cells
Concentration: 2.5, 5, 10, 20, 40, 80, 160 μg/mL
Incubation Time: 24 and 48 h
Result: Reduced cells’ viability at all concentrations for 48 h.

Western Blot Analysis[7]

Cell Line: PC12 cells
Concentration: 5, 10, 20, 40, 80, 160 μg/mL
Incubation Time: 24 h
Result: Decreased the IL-6 and IL-1β production.

RT-PCR[7]

Cell Line: PC12 cells
Concentration: 5, 10, 20 μg/mL
Incubation Time: 24 and 48 h
Result: Inhibited mRNA levels of CHRM1, HTR1A, PI3K and AKT.
Had no significant effect on the expression of mTOR.
In Vivo

Phellodendrine chloride (30-60 mg/kg, i.p., once daily for 2 weeks) inhibits macropinocytosis in mice and effectively reduces the growth of PANC-1 xenograft tumors[1].
Phellodendrine (30 mg/kg, p.o., once daily for 7 days) chloride reduces the intestinal damage of ulcerative colitis (UC) in mice[2].
Phellodendrine chloride(40 mg/kg, i.p., mice single dose or rats once daily for 5 days) alleviated Uric acid sodium (MSU) (HY-B2130A)-induced acute peritonitis in mice and arthritis in rats[3].
Phellodendrine (0.3-3 mg/kg, i.v.) chloride protects against C48/80 (HY-130592)-induced foot swelling and Evans blue exudation in mice, and suppresses C48/80-induced RBL-2H3 rat basophilic leukemia cells degranulation, and β-HEX, HIS, IL-4, and TNF-α release[4].

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

Animal Model: PANC-1 xenograft model established in Balb/c nude mice (male, 7 weeks old)[1]
Dosage: 30 and 60 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks
Result: Resulted in lower tumor weights and volumes.
Inhibited macropinocytosis in tumor tissues.
Reduced the proliferation activity of tumor cells.
Animal Model: DSS (HY-116282C) induced UC model established in female C57BL/6 mice (18-22 g)[2]
Dosage: 30 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Significantly restored the length of the colon.
Significantly reduced the disease activity index (DAI) score and the pathological damage score.
Animal Model: MSU crystal-induced arthritis model established in male Sprague-Dawley (SD) rats with a mass of 240-270 g[3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 5 days
Result: Significantly reduced the degree of joint swelling in rats.
Reduced the inflammatory score and restored the loss of proteoglycans.
Significantly inhibited the expression of MMP-3.
Animal Model: MSU induced peritonitis model established in male C57BL/6 mice (18-20 g)[3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Reduced proportion of neutrophils in the peritoneal lavage fluid.
Animal Model: C48/80-induced Hind paw swelling model established in adult male mice[4]
Dosage: 0.3 and 3 mg/kg
Administration: Intravenously injection (i.v.)
Result: Was associated with reductions in both foot swelling and the degree of Evans blue exudation in mice.
suppressed C48/80-induced RBL-2H3 rat basophilic leukemia cells degranulation, and β-HEX, HIS, IL-4, and TNF-α release.
Molecular Weight

377.86

Formula

C20H24ClNO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[N@@+]12CCC3=CC(OC)=C(O)C=C3[C@]1([H])CC4=CC(O)=C(OC)C=C4C2.[Cl-]
Structure Classification
Initial Source
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 (132.32 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 2.6465 mL 13.2324 mL 26.4648 mL
5 mM 0.5293 mL 2.6465 mL 5.2930 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.

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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: ≥ 5 mg/mL (13.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 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: 99.79%

SDS (393 KB)

COA (250 KB) LCMS (88 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 2.6465 mL 13.2324 mL 26.4648 mL 66.1621 mL
5 mM 0.5293 mL 2.6465 mL 5.2930 mL 13.2324 mL
10 mM 0.2646 mL 1.3232 mL 2.6465 mL 6.6162 mL
15 mM 0.1764 mL 0.8822 mL 1.7643 mL 4.4108 mL
20 mM 0.1323 mL 0.6616 mL 1.3232 mL 3.3081 mL
25 mM 0.1059 mL 0.5293 mL 1.0586 mL 2.6465 mL
30 mM 0.0882 mL 0.4411 mL 0.8822 mL 2.2054 mL
40 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
50 mM 0.0529 mL 0.2646 mL 0.5293 mL 1.3232 mL
60 mM 0.0441 mL 0.2205 mL 0.4411 mL 1.1027 mL
80 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
100 mM 0.0265 mL 0.1323 mL 0.2646 mL 0.6616 mL
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Keywords:

Phellodendrine104112-82-5AutophagyApoptosisAMPKmTORSTATInterleukin RelatedPKCp38 MAPKNF-κBCOXReactive Oxygen Species (ROS)PI3KAktMMPAMP-activated protein kinaseMammalian target of RapamycinILProtein kinase CNuclear factor-κBNuclear factor-kappaBCyclooxygenasePhosphoinositide 3-kinasePKBProtein kinase BMatrix metalloproteinasesKRAS mutated pancreatic cancersMacropinocytosisGlutamine metabolismMitochondrial apoptosis AutophagyNetwork pharmacologyUlcerative colitisInhibitorinhibitorinhibit

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