1. MAPK/ERK Pathway Stem Cell/Wnt Cytoskeleton Cell Cycle/DNA Damage
  2. ERK PAK
  3. Gardenin A

Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects.

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Gardenin A Chemical Structure

Gardenin A Chemical Structure

CAS No. : 21187-73-5

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Description

Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects[1][2].

In Vitro

Gardenin A (10-20 μM; 48 h) potently induces neurite outgrowth in PC12 cells, and (10 μM; 24 h and 48 h) increases expression of neuronal differentiation and synapse formation marker proteins, growth-associated protein-43 (GAP-43), and synaptophysin[1].
Gardenin A (10 μM; 30-120 min) markedly induces the phosphorylation of both cyclic AMP response element-binding protein (CREB) and CRE-mediated transcription, which was suppressed through the administration of the inhibitor 2-naphthol AS-E phosphate (KG-501) or using CREB siRNA[1].
Gardenin A (10 μM; 15-120 min) increases ERK phosphorylation and PKA and PKC activities[1].

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

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 2, 5, 10, 20 μM
Incubation Time: 48 hours
Result: showed cell growth supporting effect at higher concentrations (10-20 µM) and did not exert detectable 237 cytotoxicity on PC12 cells after 48 h incubation in low serum medium.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 10 μM
Incubation Time: 0, 15, 30, 60, and 120 min
Result: Significantly increased the phosphorylation of ERK1/2 (Thr202/Tyr204) at 15 min, subsequently reduced after 30 min.
Increased PKC and PKA activity peaked at 15 min. Increased CREB phosphorylation.
In Vivo

Gardenin A (0.1-25 mg/kg; p.o.; single dose) has neuropharmacological, including sedative, anxiolytic, antidepressant, and anticonvulsant actions in mice[2].
Gardenin A (1-10 mg/kg; p.o.; single dose) does not affect locomotor coordination in mice and delayed the onset of convulsions[2].

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

Animal Model: Male Balb/c mice (24-32 g)[2]
Dosage: 1 mg/kg, 10 mg/kg, 25 mg/kg
Administration: Oral gavage; single dose
Result: Showed sedative effects at a dose of 25 mg/kg, which increased the duration of sleep but did not alter sleep onset.
Molecular Weight

418.39

Formula

C21H22O9

CAS No.
SMILES

O=C1C=C(C2=CC(OC)=C(OC)C(OC)=C2)OC3=C(OC)C(OC)=C(OC)C(O)=C13

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    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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Gardenin A
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