1. Epigenetics TGF-beta/Smad
  2. PKC
  3. Decursinol angelate

Decursinol angelate acts as a PKC activator and GDH inhibitor, with an IC50 of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia.

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Decursinol angelate

Decursinol angelate Chemical Structure

CAS No. : 130848-06-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Decursinol angelate acts as a PKC activator and GDH inhibitor, with an IC50 of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia[1][2][3].

IC50 & Target

PKC[1].

Cellular Effect
Cell Line Type Value Description References
B16 IC50
5.8 μg/mL
Compound: 6
Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
[PMID: 22450129]
In Vitro

Decursinol angelate (20 μg/mL) exhibits cytotoxic activity across multiple human cancer cell lines with an ED50 <20 μg/mL and activates protein kinase C[1].
Decursinol angelate inhibits VEGF-induced angiogenesis in HUVECs by targeting the VEGFR2 signaling pathway[1].
Decursinol angelate potently inhibits human glutamate dehydrogenase with an IC50 of 1.432 μM[1].
Decursinol angelate inhibits melanin synthesis in B16 murine melanoma cells[1].
Decursinol angelate potently inhibits androgen receptor signaling in vitro, but is rapidly metabolized to the less active decursinol in vivo[1].
Decursinol angelate downregulates cytochrome P450 2A6 activity in human liver microsomes[1].
Decursinol angelate (20-40 μM) inhibits the expression and secretion of pro-inflammatory cytokines IL-1β and IL-6 in PMA-differentiated HL-60 cells, with no effect on IL-4 or IL-10 expression[3].
Decursinol angelate (20-40 μM) inhibits PMA-induced activation of the NFκB pathway and Raf-ERK MAPK pathway (but not the p38/JNK pathway) in PMA-differentiated HL-60 and Raw 264.7 cells[3].
Decursinol angelate (30 μM; 24 h) inhibits LPS-induced pro-inflammatory cytokine production, M1 marker expression, and macrophage polarization in Raw 264.7 cells[3].
Decursinol angelate (20-40 μM) inhibits LPS-induced NFκB translocation and MAPK pathway activation in Raw 264.7 cells[3].

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

Western Blot Analysis[3]

Cell Line: LPS-stimulated mouse macrophage Raw 264.7 cells
Concentration: 30-40 μM (NFκB translocation Western blot); 20-40 μM (MAPK pathway Western blot)
Incubation Time: null (NFκB translocation Western blot; MAPK pathway Western blot)
Result: Blocked LPS-induced activation of NFκB subunits p50 and p65.
Inhibited LPS-induced translocation of NFκB p65 from the cytoplasm to the nucleus.
Inhibited LPS-induced activation of the MAPK pathway, reducing phosphorylation of p38, ERK, and JNK.
In Vivo

Decursinol angelate (50-100 mg/kg; i.p.; daily; 9 consecutive days) dose-dependently increases the life span of mice bearing intraperitoneal Sarcoma-180 ascitic tumors, with 44.2% and 52.7% increases at 50 mg/kg and 100 mg/kg, respectively[2].
Decursinol angelate (50-100 mg/kg; i.p.; daily; 9 consecutive days) inhibits the growth of subcutaneous Sarcoma-180 solid tumors in mice, producing 39.5-40.6% tumor volume reduction and 31.0-35.2% tumor weight reduction at 50 mg/kg and 100 mg/kg, respectively[2].

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

Animal Model: ICR mice (male, 4-week-old, 23±2 g, intraperitoneally inoculated with Sarcoma-180 ascitic tumor cells)[2]
Dosage: 50 mg/kg; 100 mg/kg
Administration: i.p.; daily; 9 consecutive days
Result: Increased median survival time to 32.3 days, corresponding to a 44.2% increase in life span .
Increased median survival time to 34.2 days, corresponding to a 52.7% increase in life span .
Animal Model: ICR mice (male, 4-week-old, 23±2 g, subcutaneously transplanted with Sarcoma-180 solid tumor cells)[2]
Dosage: 50 mg/kg; 100 mg/kg
Administration: i.p.; daily; 9 consecutive days
Result: Reduced solid Sarcoma-180 tumor volume by 39.5% to 3768.8 mm3 and reduced tumor weight by 35.2% to 4.6 g.
Reduced solid Sarcoma-180 tumor volume by 40.6% to 3700.3 mm3 and reduced tumor weight by 31.0% to 4.9 g.
Molecular Weight

328.36

Formula

C19H20O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C/C=C(C)\C(O[C@H]1CC(C=C(C=CC(O2)=O)C2=C3)=C3OC1(C)C)=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 : 100 mg/mL (304.54 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 3.0454 mL 15.2272 mL 30.4544 mL
5 mM 0.6091 mL 3.0454 mL 6.0909 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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 (7.61 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.61 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 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).

*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: 99.94%

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 3.0454 mL 15.2272 mL 30.4544 mL 76.1360 mL
5 mM 0.6091 mL 3.0454 mL 6.0909 mL 15.2272 mL
10 mM 0.3045 mL 1.5227 mL 3.0454 mL 7.6136 mL
15 mM 0.2030 mL 1.0151 mL 2.0303 mL 5.0757 mL
20 mM 0.1523 mL 0.7614 mL 1.5227 mL 3.8068 mL
25 mM 0.1218 mL 0.6091 mL 1.2182 mL 3.0454 mL
30 mM 0.1015 mL 0.5076 mL 1.0151 mL 2.5379 mL
40 mM 0.0761 mL 0.3807 mL 0.7614 mL 1.9034 mL
50 mM 0.0609 mL 0.3045 mL 0.6091 mL 1.5227 mL
60 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2689 mL
80 mM 0.0381 mL 0.1903 mL 0.3807 mL 0.9517 mL
100 mM 0.0305 mL 0.1523 mL 0.3045 mL 0.7614 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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Decursinol angelate
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