1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. Corynoxeine

Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.

For research use only. We do not sell to patients.

Corynoxeine Chemical Structure

Corynoxeine Chemical Structure

CAS No. : 630-94-4

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Based on 4 publication(s) in Google Scholar

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Description

Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

Corynoxeine is able to inhibit the PDGF-BB-stimulated proliferation of VSMCs through downregulation of PDGF-BB-induced ERK1/2 activation. Pre-incubation of VSMCs with Corynoxeine significantly inhibits PDGF-BB-induced extracellular signal-regulated kinase 1/2 (ERK1/2) activation, whereas Corynoxeine has no effects on mitogen-activated protein kinase (MAPK/ERK)-activating kinase 1 and 2 (MEK1/2), Akt, or phospholipase C (PLC) γ 1 activation or on PDGF receptor beta (PDGF-Rβ) phosphorylation. Corynoxeine inhibits PDGF-BB-induced ERK1/2 activation, in the same concentration range that inhibits VSMC proliferation and DNA synthesis. Corynoxeine inhibits VSMC numbers in response to PDGF-BB with 50% inhibitory concentrations (IC50) of 13.7 μM. Corynoxeine inhibits DNA synthesis in response to PDGF-BB (24 h) with IC50 of 9.2 μM. Pre-treatment of VSMCs with Corynoxeine (5-50 μM) for 24 h results in significant decreases in cell number without any cytotoxicity; the inhibition percentages are 25.0±12.5, 63.0±27.5 and 88.0±12.5% at 5, 20 and 50 μM, respectively. Corynoxeine also significantly inhibits the 50 ng/mL PDGF-BB-induced DNA synthesis of VSMCs in a concentration-dependent manner without any cytotoxicity; the inhibitions are 32.8±11.0, 51.8±8.0 and 76.9±7.4% at concentrations of 5, 20 and 50 μM, respectively[1].

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

Molecular Weight

382.45

Formula

C22H26N2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=C2C=CC=C1)[C@]32[C@@](C[C@H](/C(C(OC)=O)=C\OC)[C@@H](C=C)C4)([H])N4CC3

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 3.8 mg/mL (9.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6147 mL 13.0736 mL 26.1472 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.93%

References
Cell Assay
[1]

Cell proliferation and DNA synthesis are measured. For cell counting, VSMCs are seeded in 12-well culture plates at 5-6×104 cells/mL and cultured in DMEM with 10% FBS at 37°C for 24 h. Under these conditions, the cells reach 70% confluence. The medium is then replaced by serum-free medium with Corynoxeine (5-50 μM). The cells are stimulated with 50 ng/mL PDGF-BB, then trypsinized with trypsin-EDTA and counted using a hemocytometer under a microscope. For [3H]-thymidine incorporation experiments, VSMCs are seeded in 24-well culture plates 5000 cells/well and then allowed to grow for 3-4 d in DMEM, and 2 μCi/mL of [3H]-thymidine are added to the medium. The reactions are terminated after 4 h by aspirating the medium and subjecting the cultures to sequential washes on ice with PBS containing 10% trichloroacetic acid and ethanol/ether (1 : 1, v/v). Acid-insoluble [3H]-thymidine is extracted into 250 μL of 0.5 M NaOH/well; this solution is then mixed with 3ml of scintillation cocktail and quantified using a liquid scintillation counter[1].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6147 mL 13.0736 mL 26.1472 mL 65.3680 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL 13.0736 mL
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Corynoxeine 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.

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Corynoxeine
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HY-N0590
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