2. GPCR/G Protein Immunology/Inflammation NF-κB Apoptosis
  3. Leukotriene Receptor NO Synthase NF-κB COX TNF Receptor Interleukin Related
  4. Tryptanthrin

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

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Tryptanthrin Chemical Structure

Tryptanthrin Chemical Structure

CAS No. : 13220-57-0

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Based on 2 publication(s) in Google Scholar

Tryptanthrin Related Antibodies

Top Publications Citing Use of Products

View All Leukotriene Receptor Isoform Specific Products:

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α[1][2].

IC50 & Target[1]

IL-2

 

nNOS

 

IL-6

 

IL-10

 

IL-12

 

In Vitro

Tryptanthrin (0-60 μM; 24, 48 and 72 h) inhibits the proliferation and colony formation of MCF-7 cells[1].
Tryptanthrin (6.25-25 μM; 48 h; MCF-7 cells) reverses EMT-associated E-cadherin, MMP-2 and Snail[1].
Tryptanthrin (0-30 μM; 15 min; MCF-7 cells) reduces Leukotriene (LT)-formation in human neutrophils with an IC50 value of 0.6 μM[2].

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

Tryptanthrin Related Antibodies

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0-60 μM
Incubation Time: 24, 48 and 72 hours
Result: Increased the inhibition rates of MCF-7 cells in a dose- and time- dependent manner.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 6.25, 12.5, and 25 μM
Incubation Time: 48 hours
Result: Increased the E-cadherin protein levels and markedly upregulated the protein expression levels of MMP-2 and Snail in MCF-7 cells induced by TGF-β1.
In Vivo

Tryptanthrin (25-100 mg/kg; i.g.; daily, for 13 d; Female Bal b/c mice with 4T1 xenograft) inhibits tumor growth and regulates IL-2, IL-6, IL-10, IL-12 and TNF-α levels in tumor-bearing mice[1].
Tryptanthrin (10 mg/kg; p.o.; male Wistar Han rats) inhibits LTB4 formation in vivo[2].

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

Animal Model: Female Bal b/c mice with 4T1 xenograft[1]
Dosage: 25, 50, and 100 mg/kg
Administration: Oral gavage; daily, for 13 days
Result: Inhibited tumor growth in a dose-dependent manner.
Animal Model: Male Wistar Han rats (220–230 g)[2]
Dosage: 10 mg/kg
Administration: Oral administration; once
Result: Reduced LTB4 pleural levels by 46%.
Reduced PGE2 levels (by 42%), exudate volume (by 80%) and the number of infiltrating cells (by 41%).
Molecular Weight

248.24

Formula

C15H8N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC=CC=C2N3C(C4=CC=CC=C4N=C13)=O
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 : 7.14 mg/mL (28.76 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 4.0284 mL 20.1418 mL 40.2836 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 0.71 mg/mL (2.86 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.71 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 0.67 mg/mL (2.70 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

COA (255 KB) LCMS (266 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, 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 4.0284 mL 20.1418 mL 40.2836 mL 100.7090 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL 20.1418 mL
10 mM 0.4028 mL 2.0142 mL 4.0284 mL 10.0709 mL
15 mM 0.2686 mL 1.3428 mL 2.6856 mL 6.7139 mL
20 mM 0.2014 mL 1.0071 mL 2.0142 mL 5.0354 mL
25 mM 0.1611 mL 0.8057 mL 1.6113 mL 4.0284 mL
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Tryptanthrin 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:

Tryptanthrin13220-57-0Leukotriene ReceptorNO SynthaseNF-κBCOXTNF ReceptorInterleukin RelatedNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBCyclooxygenaseTumor Necrosis Factor ReceptorTNFRILindole quinazolineindigo-bearing plantsLeukotriene biosynthesisanticancerMCF-7 cellsInhibitorinhibitorinhibit

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