2. NF-κB Immunology/Inflammation Apoptosis Autophagy
  3. NF-κB NOD-like Receptor (NLR) Apoptosis Autophagy
  4. Ergolide

Ergolide is an orally active dual inhibitor targeting NF-κB/p65 and NLRP3. Ergolide blocks the NF-κB signaling pathway and the nuclear translocation of p65, and irreversibly binds to the NACHT domain of NLRP3 to inhibit inflammasome assembly. Ergolide significantly reduces the production of inflammatory mediators (e.g., NO, PGE2) and cytokines, induces cancer cell apoptosis, autophagy and ROS generation. Ergolide also enhances the anti-tumor effect of vincristine. Ergolide alleviates acute lung injury via an NLRP3-dependent mechanism, and effectively improves the survival rate and behavioral function of septic mice and inflammatory zebrafish models. Ergolide is used in the research of metastatic uveal melanoma, neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease), sepsis and acute lymphoblastic leukemia.

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Ergolide

Ergolide Chemical Structure

CAS No. : 54999-07-4

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

Ergolide Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

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Description

Ergolide is an orally active dual inhibitor targeting NF-κB/p65 and NLRP3. Ergolide blocks the NF-κB signaling pathway and the nuclear translocation of p65, and irreversibly binds to the NACHT domain of NLRP3 to inhibit inflammasome assembly. Ergolide significantly reduces the production of inflammatory mediators (e.g., NO, PGE2) and cytokines, induces cancer cell apoptosis, autophagy and ROS generation. Ergolide also enhances the anti-tumor effect of vincristine. Ergolide alleviates acute lung injury via an NLRP3-dependent mechanism, and effectively improves the survival rate and behavioral function of septic mice and inflammatory zebrafish models. Ergolide is used in the research of metastatic uveal melanoma, neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease), sepsis and acute lymphoblastic leukemia[1][2][3][4][5].
IC50 & Target

p65

 

NLRP3

 

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
0.07 μM
Compound: 11
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated for 30 mins before LPS challenge measured 24 hrs after LPS challenge by Griess reaction method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated for 30 mins before LPS challenge measured 24 hrs after LPS challenge by Griess reaction method
[PMID: 21924800]
RAW264.7 IC50
3.9 μM
Compound: 16
Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
[PMID: 21894898]
In Vitro

Ergolide (0.5-10 μM; 96 h) inhibits the metabolism/viability of OMM2.5 metastatic uveal melanoma cells with an IC50 of 2.9 μM, and suppresses the long-term proliferation of both primary (Mel285, Mel270) and metastatic (OMM2.5) uveal melanoma cells[1].
Ergolide (2.5 μM; 24 h) induces reverse differential expression of BCCIP and CHID1 in OMM2.5 cells and their secreted extracellular vesicles (EVs), upregulating these proteins inside the cells while downregulating them in EVs[1].
Ergolide (5 μM; 24 h) reduces the production of nitrite, TNFα, IL-6 and MCP1 induced by LTA and LPS in BV2 microglia[2].
Ergolide (5, 10 μM; 24 h) reduces the viability and enhances the cytotoxicity of human SH-SY5Y neuroblastoma cells; at a concentration of 5 μM, it exacerbates tBHP-induced ROS production in mouse N2a cells and fails to protect SH-SY5Y cells against H2O2-induced cell death[2].
Ergolide (1-5 μM; 30 min) dose-dependently inhibits pyroptosis in mouse bone marrow-derived macrophages (BMDMs) treated with LPS + ATP[3].
Ergolide (0.5-10 μM; 18 h) reduces the expressions of iNOS, COX-2 proteins and iNOS mRNA in LPS/IFN--stimulated RAW 264.7 macrophages in a concentration-dependent manner, and inhibits IκB-α degradation after 18 h of incubation[4].
Ergolide (0-6 μM; 48 h) induces G0/G1 cell cycle arrest in Nalm6 and MOLT-4 acute lymphoblastic leukemia cell lines at 48 h, and upregulates the expression of cell cycle inhibitory genes p21 and p27, with no effect on non-tumorigenic PBMC[5].
Ergolide (2-4 μM; 24-48 h) induces ROS-dependent autophagy in MOLT-4 acute lymphoblastic leukemia cells at 24 h by upregulating autophagy-related genes and genes in the Sirt1-Bnip3-FoxO3a pathway; in addition, autophagy acts as a survival pathway, and inhibition of autophagy enhances Ergolide-induced apoptosis[5].

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

Ergolide Related Antibodies

Western Blot Analysis[4]

Cell Line: RAW 264.7 macrophages (LPS/IFN-γ-stimulated)
Concentration: 0.5-10 μM
Incubation Time: 18 h
Result: Decreased iNOS protein levels in a concentration-dependent manner, with significant inhibition observed at 2, 5, and 10 μM.\n
Decreased COX-2 protein levels in a concentration-dependent manner, with significant inhibition observed at 2, 5, and 10 μM.

Cell Cycle Analysis[5]

Cell Line: Human leukemic cell lines (Nalm6, MOLT-4); non-tumorous PBMC
Concentration: 0-6 μM (cell cycle analysis); 4 μM (qRT-PCR for gene expression)
Incubation Time: 48 h (cell cycle analysis; qRT-PCR for gene expression)
Result: Induced G0/G1 phase arrest in Nalm6 and MOLT-4 cells, with no significant arrest in non-tumorous PBMC.
Increased mRNA expression of p21 and p27 in Nalm6 and MOLT-4 cells:
Nalm6 p21: ~4.5-fold change,
Nalm6 p27: ~2.8-fold change,
MOLT-4 p21: ~3.2-fold change,
MOLT-4 p27: ~2.7-fold change.
Increased Sub-G1 population (apoptotic cells) in Nalm6 and MOLT-4 cells.

Apoptosis Analysis[5]

Cell Line: Human leukemic cell lines (Nalm6, MOLT-4)
Concentration: 2-6 μM (8 h ROS measurement; 48 h apoptosis analysis); 4-6 μM with 10 mM NAC pre-treatment (8 h ROS measurement, 48 h cell death assay); 6 μM (48 h Bax/Bcl-2 gene expression)
Incubation Time: 8 h (ROS measurement); 48 h (apoptosis analysis, cell death assay, gene expression)
Result: Dose-dependently increased ROS levels in Nalm6 (up to 2-fold) and MOLT-4 (up to 4-fold) cells; NAC pre-treatment abrogated ergolide-induced ROS accumulation and reduced cell death in MOLT-4 cells.

Dose-dependently increased apoptotic cell death:
Nalm6: ~80% cell death at 6 μM,
MOLT-4: ~40% cell death at 6 μM.

Increased Bax mRNA expression (~3.8-fold change) and decreased Bcl-2 mRNA expression (~0.3-fold change) in Nalm6 cells treated with 6 μM ergolide; similar changes observed in MOLT-4 cells.
In Vivo

Ergolide (2.5 μM; 3 d) exerts significant in vivo anticancer effects in a zebrafish OMM2.5 xenograft model, reducing the normalized mean fluorescence of primary xenografts by 56% without altering the number of disseminated cells[1].
Ergolide (incubated in embryo culture medium; pre-treatment for 23.5 h + 30 min) increases the survival rate, restores sensorimotor function, and reduces the expression of il-1β in LPS-stimulated zebrafish larvae; however, it fails to alleviate pentylenetetrazol (PTZ)-induced epileptiform hyperactivity in zebrafish larvae at 15 mM[2].
Ergolide (5-10 mg/kg; p.o.; once every 2 days; for 7 consecutive days) dose-dependently improves the survival rate of male C57BL/6J mice with sepsis, alleviates LPS-induced acute lung injury in wild-type mice in an NLRP3-dependent manner, but no protective effect is observed in NLRP3-knockout mice[3].

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

Animal Model: WT-Tü Zebrafish (4-5 days post-fertilisation larvae; LPS-induced systemic inflammation model)[2]
Dosage: 3 μM; 5 μM
Administration: incubated in embryo media; 24 h total
Result: Significantly increased the survival rate of LPS-challenged larvae compared to LPS alone at 5 μM.
Significantly restored the LPS-impaired touch startle response, increasing the proportion of larvae exhibiting an escape-like reflex movement at 5 μM.
Significantly reduced LPS-induced upregulation of il-1β mRNA expression in larvae at 5 μM, but did not alter LPS-induced increases in tnfα or il-8 mRNA expression.
Significantly increased tnfα mRNA expression in unchallenged larvae at 5 μM.
Animal Model: C57BL/6J (male) mice[3]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.g.; every 2 days; 7 days
Result: Showed a higher survival rate in the 10 mg/kg group than the 5 mg/kg group.
Prevented all mice from dying within 48 hours, with a portion surviving through the 72-hour observation period in both treated groups.
Animal Model: C57BL/6J wild-type (male) mice; C57BL/6-Nlrp3-/- (NLRP3 knockout, male) mice[3]
Dosage: 10 mg/kg
Administration: i.g.; every 2 days; 7 days
Result: Significantly reduced LPS-induced lung injury scores, myeloperoxidase (MPO) activity in lung tissue, lung wet/dry weight ratio, total cell count, total protein concentration, and neutrophil count in BALF, as well as IL-1β levels in serum and BALF in wild-type mice.
Reduced the expression of mature IL-1β and cleaved caspase-1 (P20) in wild-type mouse lung tissue.
Produced no significant beneficial effects in NLRP3 knockout mice.
Molecular Weight

306.35

Formula

C17H22O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(O[C@@H]1[C@]2([C@](CCC2=O)([H])[C@H](C)C[C@@](O3)([H])[C@@]1([H])C(C3=O)=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 : 50 mg/mL (163.21 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 3.2642 mL 16.3212 mL 32.6424 mL
5 mM 0.6528 mL 3.2642 mL 6.5285 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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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.16 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.
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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: 99.48%

SDS (252 KB)

COA (254 KB) HNMR (273 KB) LCMS (92 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, 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 3.2642 mL 16.3212 mL 32.6424 mL 81.6060 mL
5 mM 0.6528 mL 3.2642 mL 6.5285 mL 16.3212 mL
10 mM 0.3264 mL 1.6321 mL 3.2642 mL 8.1606 mL
15 mM 0.2176 mL 1.0881 mL 2.1762 mL 5.4404 mL
20 mM 0.1632 mL 0.8161 mL 1.6321 mL 4.0803 mL
25 mM 0.1306 mL 0.6528 mL 1.3057 mL 3.2642 mL
30 mM 0.1088 mL 0.5440 mL 1.0881 mL 2.7202 mL
40 mM 0.0816 mL 0.4080 mL 0.8161 mL 2.0402 mL
50 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6321 mL
60 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3601 mL
80 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0201 mL
100 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8161 mL
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Ergolide 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:

Ergolide54999-07-4NF-κBNOD-like Receptor (NLR)ApoptosisAutophagyNuclear factor-κBNuclear factor-kappaBNLRP3 inflammasomeRAW 264.7 macrophagesIκB-αBV2 microglial cellsacute lymphoblastic leukemia cell linesseptic miceNACHT domainzebrafishp65Inhibitorinhibitorinhibit

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