2. Membrane Transporter/Ion Channel Epigenetics Cell Cycle/DNA Damage Anti-infection PI3K/Akt/mTOR Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. GLUT HDAC Virus Protease PI3K AMPK Akt Histone Demethylase MDM-2/p53 IFNAR Reactive Oxygen Species (ROS)
  4. Deoxyandrographolide

Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection.

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Deoxyandrographolide

Deoxyandrographolide Chemical Structure

CAS No. : 79233-15-1

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Deoxyandrographolide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Deoxyandrographolide

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GLUT1 GLUT2 GLUT3 GLUT4

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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Akt Akt1 Akt2 Akt3

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection[3].

IC50 & Target[1]

GLUT4

 

HDAC1

38.4 μM ()

In Vitro

Deoxyandrographolide (2.5-25 μM; 1-24 h) dose- and time-dependently stimulates glucose uptake in L6 myotubes, and its effects are additive to Insulin without reducing cell viability[1].
Deoxyandrographolide (10 μM; 16 h) does not alter total cellular GLUT4 or GLUT1 protein levels in L6 myotubes, either alone or in combination with Insulin[1].
Deoxyandrographolide (10-25 μM; 16 h) dose-dependently promotes GLUT4 translocation to the plasma membrane in L6-GLUT4myc myotubes, with a 1.23-fold increase at 25 μM for 16 h, and potentiates Insulin-induced GLUT4 translocation[1].
Deoxyandrographolide (10 μM; 16 h) stimulates glucose uptake in L6 myotubes via a PI-3-K-dependent pathway, and activates downstream signaling by increasing Akt and insulin receptor-β phosphorylation, with synergistic effects when combined with insulin[1].
Deoxyandrographolide (10-25 μM; 16 h) activates the AMPK pathway in L6 myotubes, as shown by increased AMPKα and ACC phosphorylation, and this pathway contributes to its ability to promote GLUT4 translocation[1].
Deoxyandrographolide (7.94-250 μM; 24 h) is non-toxic to rat aorta endothelial cells at concentrations up to 200 μM and to human microvascular endothelial cells at concentrations up to 125 μM after 24 h of incubation[2].
Deoxyandrographolide (50-150 μM; 48 h) inhibits Angiotensin II-induced upregulation of p16 and p21 mRNA in rat aorta endothelial cells and human microvascular endothelial cells[2].
Deoxyandrographolide (25-150 μM; 48 h) inhibits Angiotensin II-induced p53 upregulation in rat aorta endothelial cells, restores angiotensin II-reduced HDAC1 levels in human microvascular endothelial cells, and reduces Angiotensin II-induced H3K4me3 upregulation in rat aorta endothelial cells[2].
Deoxyandrographolide (50-100 μM; 48-60 h) at 50 and 100 μM reduces angiotensin II-induced γH2A.X and p21 upregulation, and at 100 μM reduces angiotensin II-induced ubiquitin upregulation in rat aorta endothelial cells[2].
Deoxyandrographolide (6.75-200 μM) binds directly to recombinant human HDAC1 protein with a KD of 38.4 μM, as measured by bio-layer interferometry[2].
Deoxyandrographolide (50-150 μM; 24 h) reduces angiotensin II-induced reactive oxygen species accumulation in wild-type rat aorta endothelial cells, but this effect is abolished in HDAC1-knockdown rat aorta endothelial cells[2].
Deoxyandrographolide (50-150 μM; 48 h) fails to inhibit angiotensin II-induced γH2A.X upregulation in HDAC1-knockdown rat aorta endothelial cells[2].
Deoxyandrographolide (100 μM; 48 h) modulates gene expression related to chromosome stability, cell cycle, senescence, and inflammation in angiotensin II-treated rat aorta endothelial cells[2].
Deoxyandrographolide (1-150 μM; 24 h) inhibits replication of FMDV serotype A in BHK-21 cells with an EC50 of 36.47 μM and a selective index of 9.22[3].
Deoxyandrographolide (1-100 μM; 16 h) inhibits the protease activity of FMDV 3Cpro in HEK 293T cells with an IC50 of 25.58 μM and IC90 of 122.88 μM[3].
Deoxyandrographolide (25.58-122.88 μM; 24 h) interferes with the IFN-antagonist activity of FMDV 3Cpro in HEK 293T cells, significantly upregulating the expression of interferon-stimulating genes ISG15, ISG56, Mx-1, OAS-1, and PKR[3].
Deoxyandrographolide (0.1-250 μM; 24 h) exhibits mild cytotoxicity in BHK-21 cells (CC50 = 332.3 μM) and HEK 293T cells (CC50 = 651.40 μM) with non-cytotoxic CC10 concentrations of 81.05 μM and 155.55 μM, respectively[3].

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

Deoxyandrographolide Related Antibodies

Western Blot Analysis[1]

Cell Line: L6 myotubes
Concentration: 10 μM
Incubation Time: 16 h
Result: Increased p-Akt and P-TRβ expression.
Increased p-AMPK and P-ACC expression.

Cell Viability Assay[2]

Cell Line: rat aorta endothelial cells (RaECs), human microvascular endothelial cells (HMEC-1)
Concentration: 12.5, 25, 50, 10, 200 μM (RaECs); 7.94, 15.88, 31.75, 62.5, 125, 250 μM (HMEC-1)
Incubation Time: 24 h
Result: Showed no significant cytotoxicity in RaECs at concentrations up to 200 μM.
Showed no significant cytotoxicity in HMEC-1 at concentrations up to 125 μM; cytotoxicity was observed at 250 μM.

RT-PCR[2]

Cell Line: rat aorta endothelial cells (RaECs), human microvascular endothelial cells (HMEC-1)
Concentration: 50, 100, 150 μM
Incubation Time: 48 h (co-incubated with 2 μM Ang II)
Result: Dose-dependently inhibited the Ang II-induced elevation of p16 and p21 mRNA levels in both RaECs and HMEC-1.

Western Blot Analysis[2]

Cell Line: rat aorta endothelial cells (RaECs), human microvascular endothelial cells (HMEC-1)
Concentration: 50, 100, 150 μM (p53 and HDAC1 assays); 25, 50, 100, 150 μM (H3K4me3 assay)
Incubation Time: 48 h (co-incubated with 2 μM Ang II)
Result: Inhibited Ang II-induced upregulation of p53 protein in RaECs at 50, 100, and 150 μM.
Dose-dependently restored HDAC1 protein levels reduced by Ang II in HMEC-1 at 50, 100, and 150 μM.
Dose-dependently downregulated H3K4me3 levels increased by Ang II in RaECs at 25, 50, 100, and 150 μM.

Immunofluorescence[2]

Cell Line: rat aorta endothelial cells (RaECs)
Concentration: 50, 100 μM (γH2A.X and p21 assays); 100 μM (ubiquitin assay)
Incubation Time: 48 h (γH2A.X and p21 assays; co-incubated with 2 μM Ang II); 60 h (ubiquitin assay; co-incubated with 2 μM Ang II)
Result: Reduced Ang II-induced elevation of γH2A.X and p21 fluorescence intensity at 50 and 100 μM.
Decreased Ang II-induced elevation of total ubiquitin fluorescence intensity at 100 μM.

Cell Cytotoxicity Assay[3]

Cell Line: BHK-21, HEK 293T
Concentration: 0.1,
1, 5, 10, 25, 50, 75, 100, 200, and 250 μM
Incubation Time: 24 h
Result: In BHK-21 cells, reached a CC50 of 332.3 μM and a CC10 of 81.05 μM.
In HEK 293T cells, reached a CC50 of 651.40 μM and a CC10 of 155.55 μM, indicating mild cytotoxicity only at high concentrations.
In Vivo

Deoxyandrographolide (100 mg/kg; p.o.; single dose) produces significant antihyperglycemic activity in Streptozotocin (HY-13753)-induced diabetic rats, lowering blood glucose by 20.2% at 5 hours and 24.3% at 24 hours[1].
Deoxyandrographolide (100 mg/kg; p.o.; daily; 15 days) significantly reduces blood glucose, improves glucose tolerance, and normalizes lipid and insulin profiles in genetically diabetic db/db mice, including a 36.6% improvement in fasting blood glucose[1].

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

Animal Model: Sprague Dawley (male, 160 g, Streptozotocin-induced diabetic)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Reduced blood glucose by 20.2% at 5 hours post-dose.
Reduced blood glucose by 24.3% at 24 hours post-dose, as measured by AUC comparison to vehicle controls.
Animal Model: C57BL/KsJ-db/db (male, 40 g, genetically diabetic)[1]
Dosage: 100 mg/kg
Administration: p.o.; daily; 15 days
Result: Reduced blood glucose significantly starting on day 11, continuing through day 14.
Improved glucose tolerance by 16.1% on day 10 and 23.4% on day 15 via OGTT.
Improved fasting blood glucose by 36.6%.
Reduced serum insulin by 29.9%.
Decreased serum triglycerides by 15.3%.
Decreased LDL-cholesterol by 13.1%.
Increased HDL-cholesterol by 23.4%.
Caused no significant effect on total cholesterol or body weight.
Molecular Weight

334.45

Formula

C20H30O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@](C(CCC1=CCOC1=O)=C(C)CC2)(CC[C@H]3O)[C@@]2([H])[C@]3(C)CO
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 (299.00 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 2.9900 mL 14.9499 mL 29.8998 mL
5 mM 0.5980 mL 2.9900 mL 5.9800 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

Concentration (start)

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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 (7.47 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.47 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:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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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
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 2.9900 mL 14.9499 mL 29.8998 mL 74.7496 mL
5 mM 0.5980 mL 2.9900 mL 5.9800 mL 14.9499 mL
10 mM 0.2990 mL 1.4950 mL 2.9900 mL 7.4750 mL
15 mM 0.1993 mL 0.9967 mL 1.9933 mL 4.9833 mL
20 mM 0.1495 mL 0.7475 mL 1.4950 mL 3.7375 mL
25 mM 0.1196 mL 0.5980 mL 1.1960 mL 2.9900 mL
30 mM 0.0997 mL 0.4983 mL 0.9967 mL 2.4917 mL
40 mM 0.0747 mL 0.3737 mL 0.7475 mL 1.8687 mL
50 mM 0.0598 mL 0.2990 mL 0.5980 mL 1.4950 mL
60 mM 0.0498 mL 0.2492 mL 0.4983 mL 1.2458 mL
80 mM 0.0374 mL 0.1869 mL 0.3737 mL 0.9344 mL
100 mM 0.0299 mL 0.1495 mL 0.2990 mL 0.7475 mL
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Deoxyandrographolide Related Classifications

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  • 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:

Deoxyandrographolide79233-15-1GLUTHDACVirus ProteasePI3KAMPKAktHistone DemethylaseMDM-2/p53IFNARReactive Oxygen Species (ROS)Glucose transporter Histone deacetylasesPhosphoinositide 3-kinaseAMP-activated protein kinasePKBProtein kinase BInterferon-α/β receptorInterferon-alpha/beta receptorHEK 293T cellsrat aorta endothelial cellsGLUT4Foot-and-Mouth Disease Virus 3CproL6 myotubesPI-3-Khuman microvascular endothelial cellsBHK-21 cellsHDAC1Inhibitorinhibitorinhibit

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