1. Protein Tyrosine Kinase/RTK
    Apoptosis
    Anti-infection
  2. Src
    Apoptosis
    Fungal
  3. Damnacanthal

Damnacanthal 

Cat. No.: HY-108485 Purity: >98.0%
Handling Instructions

Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.

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

Damnacanthal Chemical Structure

Damnacanthal Chemical Structure

CAS No. : 477-84-9

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1][2][3][4].

IC50 & Target

IC50: 46 nM (p56 lck autophosphorylation) and 220 nM (phosphorylation of exogenous substrates by p56 lck)[1];
Apoptosis[2];
Candida albicans[2]

In Vitro

Damnacanthal has > 100-fold selectivity for p56lck over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56lck over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56lck over the homologous enzymes p60src and p59fyn[1].
Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner[2].
Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM[2].
Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis[2].
Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced[2].
Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner[2].

Cell Proliferation Assay[2]

Cell Line: HCT-116 and SW480 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 1, 2, and 4 days
Result: Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner.

Cell Cycle Analysis[2]

Cell Line: HCT-116 cells
Concentration: 1 μM, 10 μM and 50 μM
Incubation Time: 72 hours
Result: Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.

Apoptosis Analysis[2]

Cell Line: HCT-116 cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Significantly increased caspase 3/7 activity.

Western Blot Analysis[2]

Cell Line: HCT-116 cells
Concentration: 0.1 μM, 1 μM and 10 μM
Incubation Time: 24 hours
Result: NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM.
In Vivo

Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema[4].

Animal Model: Male ddY mice (5-6 weeks) injected with formalin or Histamine[4]
Dosage: 10 mg/kg, 30 mg/kg and 100 mg/kg
Administration: Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result: Significantly reduced the growth of human lung tumor without acute toxicity.
Molecular Weight

282.25

Formula

C₁₆H₁₀O₅

CAS No.

477-84-9

SMILES

O=CC(C(OC)=C1C2=O)=C(O)C=C1C(C3=C2C=CC=C3)=O

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)

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

DamnacanthalSrcApoptosisFungalNaturalantinociceptivecanceranti-fungalp56lcktyrosinekinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Damnacanthal
Cat. No.:
HY-108485
Quantity:
MCE Japan Authorized Agent: