2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis Anti-infection
  3. Carboxylesterase (CES) DNA/RNA Synthesis Apoptosis Bacterial
  4. Nevadensin

Nevadensin (Lysionotin), a natural flavonoid, is a selective human carboxylesterase 1 (hCE1) inhibitor with an IC50 of 2.64 μM. Nevadensin is more selective for hCE1 than hCE2 (IC50 of 132.8 μM). Nevadensin can induce apoptosis and DNA damage in cancer cells. Nevadensin has a variety of pharmacological effects such as anti-inflammatory, anti-tumour, anti-hypertensive, anti-tubercular, antitussive, antioxidant and anti-microbial activities.

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Nevadensin Chemical Structure

Nevadensin Chemical Structure

CAS No. : 10176-66-6

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Based on 1 publication(s) in Google Scholar

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Nevadensin Related Antibodies

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Description

Nevadensin (Lysionotin), a natural flavonoid, is a selective human carboxylesterase 1 (hCE1) inhibitor with an IC50 of 2.64 μM. Nevadensin is more selective for hCE1 than hCE2 (IC50 of 132.8 μM). Nevadensin can induce apoptosis and DNA damage in cancer cells. Nevadensin has a variety of pharmacological effects such as anti-inflammatory, anti-tumour, anti-hypertensive, anti-tubercular, antitussive, antioxidant and anti-microbial activities[1][2][3][4][5].

IC50 & Target

IC50: 2.64 μM (hCE1), 132.8 μM (hCE2)[1]
In Vitro

Nevadensin exhibits inhibition activity against Mycobacterium tuberculosis, with a MIC value of 200 μg/mL. Nevadensin exhibits antioxidant activity against the radical scavenging ability of DPPH, with the IC50 value of 7.7 μg/mL[2].
Nevadensin potently inhibits p40 protein tyrosine kinase activity with an IC50 value of 50 μg/mL[3].
Nevadensin shows DNA-intercalating properties, with IC50s of 31.63 µM and 296.91 µM for minor groove binding and DNA intercalation[3].
Nevadensin (500 μM; 1 h) in human colon carcinoma cell line HT29 cells, significantly increases the amount of topoisomerase I (TOPO I) bound to DNA, but has no stabilizing effect on the TOPO IIα/DNA complex[3].
Nevadensin (1-500 μM; 24-48 h) in HT29 cells, causes a slight but significant reduction in cell viability of about 20% at concentrations ≥250 μM after 24 h, and a significant decrease in cell viability but still higher than 50% after 48 h[3].
Nevadensin (1-500 μM; 24 h) in HT29 cells, increases the number of cells in the G2/M phase at concentrations ≥100 μM[3].
Nevadensin (50-500 μM; 24 h) in HT29 cells, increases the activities of caspase-3 and caspase-9 in a concentration-dependent manner and has no effect on the activity of caspase-8[3].
Nevadensin (12.5-50 µM; for 24 h) significantly inhibits growth of hepatocellular carcinoma (HCC) cells via inducing cell cycle arrest and apoptosis. Nevadensin regulates multiple functional signaling pathways associated with cancer including Hippo signaling. Nevadensin notably induces activation of the MST1/2-LATS1/2 kinase in HCC cells[4].
Nevadensin (1-10 μg/mL) inhibits the release of β-hexosaminidase and histamine in bone marrow-derived mast cells[5].
Nevadensin (2-20 μg/mL; 3 days) in BMMCs (bone marrow-derived mast cells) inhibits cell proliferation, decreases the expression of c-Kit and accelerates their apoptosis[5].

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

Nevadensin Related Antibodies

Cell Viability Assay[3]

Cell Line: HT29 cells
Concentration: 1 μM, 10 μM, 100 μM, 250 μM, 500 μM
Incubation Time: 24 h, 48 h
Result: After 24 h, at concentrations ≥250 μM, cell viability was slightly but significantly reduced by about 20%.

Cell Cycle Analysis[3]

Cell Line: HT29 cells
Concentration: 1 μM, 10 μM, 100 μM, 250 μM, 500 μM
Incubation Time: 24 h
Result: At concentrations ≥100 μM, the number of cells in the G2/M phase increased.

Western Blot Analysis[3]

Cell Line: HT29 cells
Concentration: 50 μM, 100 μM, 250 μM, 500 μM
Incubation Time: 24 h
Result: Increased the levels of apoptosis-related proteins such as Cleaved Caspase 3, Cleaved-PARP, and Cleaved Caspase 9 in a concentration-dependent manner.
In Vivo

Nevadensin (1-10 mg/kg; gavage; once a day; from day 27 to day 40) in ovalbumin (OVA)-induced mouse food allergy model alleviates allergic symptoms and decreases the levels of serum specific immunoglobulin E, histamine, and mouse mast cell protease-1[5].

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

Animal Model: Female BALB/c mice (6-8 weeks) were sensitized through intraperitoneal injection of 100 μg of ovalbumin and 2 mg of alum in 200 μL of PBS on days 0 and 14, and then orally challenged with 50 mg of ovalbumin in 200 μL of PBS every 3 days from day 28 for a total of five challenge events[5].
Dosage: 1, 5 or 10 mg/kg
Administration: Oral gavage, once a day, from day 27 to day 40
Result: Significantly attenuated oral ovalbumin-challenge-induced food allergy, as assessed by improvements in hypothermia, diarrhea, and anaphylaxis score.
Also led to significantly decreased levels of OVA-specific IgE, histamine, and mMCP-1 in the serum.
Molecular Weight

344.32

Formula

C18H16O7
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(OC)C=C2)OC3=C(OC)C(O)=C(OC)C(O)=C13
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 14.71 mg/mL (42.72 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 2.9043 mL 14.5214 mL 29.0428 mL
5 mM 0.5809 mL 2.9043 mL 5.8085 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 (protect from light). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 2.5 mg/mL (7.26 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.93%

SDS (393 KB)

COA (249 KB) LCMS (93 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 (protect from 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 2.9043 mL 14.5214 mL 29.0428 mL 72.6069 mL
5 mM 0.5809 mL 2.9043 mL 5.8086 mL 14.5214 mL
10 mM 0.2904 mL 1.4521 mL 2.9043 mL 7.2607 mL
15 mM 0.1936 mL 0.9681 mL 1.9362 mL 4.8405 mL
20 mM 0.1452 mL 0.7261 mL 1.4521 mL 3.6303 mL
25 mM 0.1162 mL 0.5809 mL 1.1617 mL 2.9043 mL
30 mM 0.0968 mL 0.4840 mL 0.9681 mL 2.4202 mL
40 mM 0.0726 mL 0.3630 mL 0.7261 mL 1.8152 mL
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Nevadensin 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:

Nevadensin10176-66-6LysionotinCarboxylesterase (CES)DNA/RNA SynthesisApoptosisBacterialCarboxylesteraseCarboxylic-ester HydrolaseflavonoidinhibitionnaturalselectivepharmacologicaleffectInhibitorinhibitorinhibit

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