1. Anti-infection Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis
  2. Bacterial HIF/HIF Prolyl-Hydroxylase PI3K Apoptosis
  3. Deoxyshikonin

Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL).

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

Deoxyshikonin Chemical Structure

Deoxyshikonin Chemical Structure

CAS No. : 43043-74-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 240 In-stock
Solution
10 mM * 1 mL in DMSO USD 240 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 160 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Deoxyshikonin

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistant S. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL)[1][2][3].

IC50 & Target[1][2][3]

HIF-1α

 

HIF-1β

 

PI3K

 

In Vitro

Deoxyshikonin (6.25-100 μg/mL; 48 h) inhibits the growth of human colonic cancer cells[1].
Deoxyshikonin (25-100 μg/mL; 24, 48 h) induces early apoptotic cells death[1].
Deoxyshikonin (25-100 μg/mL; 48 h) leads to a dose-dependent increase in the percentage of cells at G0/G1 phase[1].
Deoxyshikonin (25-100 μg/mL; 48 h) exerts a decrease of PI3K, p-PI3K, Akt, p-Akt308 and mTOR proteins expression in HT29 and DLD-1 cell lines[1].

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

Cell Viability Assay[3]

Cell Line: Caco-2, HCT116, DLD-1 and HT29 cells
Concentration: 6.25, 12.5, 25, 50 and 100 μg/mL
Incubation Time: 48 h
Result: At low concentration inhibited the growth of human colonic cancer cells including DLD-1, HCT-116, Caco-2 and HT29 cells.
Had IC50 values of 31.00  μM at 24 h, while 10.97 μM at 48 h in HT29 cells.

Apoptosis Analysis[3]

Cell Line: HT29 cells
Concentration: 25, 50 and 100 μg/mL
Incubation Time: 24 or 48 h
Result: The ratio of early apoptotic cells increased from 1% to 29% in a dose-dependent manner by being treated with 0-50 μg/mL at 48 h.

Cell Cycle Analysis[3]

Cell Line: HT29 cells
Concentration: 25, 50 and 100 μg/mL
Incubation Time: 48 h
Result: The percentage of G0/G1 cells increased from approximately 44% to 67% in HT29 cells after treatment with 0-50 μg/mL, accompanied by a significant decrease in the percentage of cells at S and G2/M phases.

Western Blot Analysis[3]

Cell Line: HT29 and DLD-1 cell lines
Concentration: 25, 50 and 100 μg/mL
Incubation Time: 48 h
Result: Exerted a decrease of PI3K, p-PI3K, Akt, p-Akt308 and mTOR proteins expression in HT29 and DLD-1 cell lines.
In Vivo

Deoxyshikonin (20 mg/kg; intraperitoneal injection; every two days for 13 days) markedly suppresses the growth of xenograft tumours on day 5, 9 and 11 with 20 mg/kg[1].

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

Animal Model: Male BALB/c nude mice of 10-14 g with DLD-1 cells[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; every two days for a total of 13 days
Result: Markedly suppressed the growth of xenograft tumours on day 5, 9 and 11 with 20 mg/kg, while there were no significant changes in body weight of the mice.
Molecular Weight

272.30

Formula

C16H16O4

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1C(CC/C=C(C)/C)=CC(C2=C1C(O)=CC=C2O)=O

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 : 33.33 mg/mL (122.40 mM; ultrasonic and warming and heat to 60°C; 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 3.6724 mL 18.3621 mL 36.7242 mL
5 mM 0.7345 mL 3.6724 mL 7.3448 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

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

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: 99.96%

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 3.6724 mL 18.3621 mL 36.7242 mL 91.8105 mL
5 mM 0.7345 mL 3.6724 mL 7.3448 mL 18.3621 mL
10 mM 0.3672 mL 1.8362 mL 3.6724 mL 9.1811 mL
15 mM 0.2448 mL 1.2241 mL 2.4483 mL 6.1207 mL
20 mM 0.1836 mL 0.9181 mL 1.8362 mL 4.5905 mL
25 mM 0.1469 mL 0.7345 mL 1.4690 mL 3.6724 mL
30 mM 0.1224 mL 0.6121 mL 1.2241 mL 3.0604 mL
40 mM 0.0918 mL 0.4591 mL 0.9181 mL 2.2953 mL
50 mM 0.0734 mL 0.3672 mL 0.7345 mL 1.8362 mL
60 mM 0.0612 mL 0.3060 mL 0.6121 mL 1.5302 mL
80 mM 0.0459 mL 0.2295 mL 0.4591 mL 1.1476 mL
100 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9181 mL
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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.

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Deoxyshikonin
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HY-N2187
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