2. Metabolic Enzyme/Protease Anti-infection NF-κB Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling Epigenetics PI3K/Akt/mTOR
  3. HIV Integrase Bacterial Antibiotic Reactive Oxygen Species STAT AMPK 11β-HSD
  4. Equisetin

Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects.

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Equisetin Chemical Structure

Equisetin Chemical Structure

CAS No. : 57749-43-6

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Based on 1 publication(s) in Google Scholar

Equisetin Related Antibodies

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Description

Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects[1][2][3][4][5][6][7][8][9][10][11].

IC50 & Target[10]

STAT3

 

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM GI50
144 nM
Compound: 5, NSC 772378
Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition by SRB assay
Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition by SRB assay
[PMID: 24422636]
In Vitro

Equisetin (50-300 μM, 6 h) inhibit the production of virulence factor, biofilm formation, and swarming motility of Pseudomonas aeruginosa PAO1[4].
Equisetin shows cytotoxicity against human CCRF-CEM cells assessed as growth inhibition by SRB assay, with a GI50 of 144 nM[7].
Equisetin (1-6 μg/mL, 0-6 h) removes Staphylococcus aureus from IEC-6 cells by enhancing host autophagy and inducing mitochondria-mediated ROS generation[8].
Equisetin (20 μM, 7 days) inhibits adiposity through AMPK-dependent regulation of brown adipocyte (BA) differentiation[9].
Equisetin (0.01-100 μM, pre-stimulates 12 h) attenuates lipid droplet accumulation and foam cell formation in macrophages[10].
Equisetin (0.01-10 μM) inhibits LPS and oxLDL-induced inflammatory responses in macrophages (RAW264.7 and BMDM)[10].
Equisetin (4 µg/mL) can potentiate Colistin (HY-113678) activity against multi-drug resistant gram-negative bacteria including Colistin -resistant strains[11].

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

Equisetin Related Antibodies

Western Blot Analysis [9]

Cell Line: 3T3-L1
Concentration: 20 μM
Incubation Time: 7 days
Result: Increased the specific BA markers Prdm16 and the uncoupling protein Ucp1, the mitochondrial markers Pgc1α, and Tfam.
Increased AMPK and phosphorylated AMPK (pAMPK).
In Vivo

Equisetin (20-80 mg/kg, i.g., 6 weeks) inhibits obesity and increased energy expenditure in high-fat diet-induced obese mice through inhibition of the enzymatic activity of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)[5].
Equisetin (10 mg/kg, i.p., 6 h) shows significant anti-infective activity in a mouse model of Staphylococcus aureus ATCC 29213 infection[8].
Equisetin (5-20 mg/kg, p.o., every two days until 12 weeks) prevents atherosclerosis in mice by binding to and inhibiting the activity of STAT3[10].

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

Animal Model: Atherosclerosis model (eight-week-old male ApoE-/- mice were fed with HFD for 12 weeks)[10]
Dosage: 5, 20 mg/kg
Administration: Oral gavage (p.o.), every two days until 12 weeks
Result: Attenuated HFD-induced lipid area in the en face prepared aorta and aortic root.
Attenuated atherosclerotic lesion area (HFD versus HFD+5 mg/kg Equisetin: 31.71 versus 16.95; HFD versus HFD+20 mg/kg Equisetin: 31.71 versus 10.12).
Increased collagen content in the aortic plaques.
Increased α-SMA-positive areas in the plaques in aortic root.
Molecular Weight

373.49

Formula

C22H31NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(/C1=C(O)\[C@]2(C)[C@H](/C=C/C)C=C[C@]3([H])C[C@H](C)CC[C@@]23[H])N(C)[C@@H](CO)C1=O
Structure Classification
Initial Source

marine fungus Fusarium sp. Z10
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (2.68 mM; Need ultrasonic and warming; 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 2.6774 mL 13.3872 mL 26.7745 mL
5 mM --- --- ---
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. 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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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.40%

SDS (392 KB)

COA (258 KB) RP-HPLC (678 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. 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 2.6774 mL 13.3872 mL 26.7745 mL 66.9362 mL
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Equisetin 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:

Equisetin57749-43-6HIV IntegraseBacterialAntibioticReactive Oxygen SpeciesSTATAMPK11β-HSDAMP-activated protein kinase11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenaseBiofilmBrown adipocyteCCRF-CEMRAW264.7BMDMObesityAtherosclerosis.Inhibitorinhibitorinhibit

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