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  4. Caerulomycin A

Caerulomycin A  (Synonyms: Cerulomycin; Caerulomycin)

Cat. No.: HY-114495 Purity: 98.0%
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Caerulomycin A is an orally active immunomodulator and antimicrobial agent. Caerulomycin A targets Smad3, STAT1 and GATA-3. Caerulomycin A downregulates GATA-3 expression, inhibits Th2 cell differentiation and Th2 cytokine production, reduces IgE levels, and alleviates pulmonary inflammatory responses and eosinophil infiltration. Caerulomycin A ameliorates collagen-induced arthritis symptoms, reduces joint inflammation and synovitis, and decreases the levels of proinflammatory cytokines in joints. Caerulomycin A inhibits the growth of some filamentous fungi, yeasts and specific bacteria. Caerulomycin A can be used in research related to arthritis and asthma.

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

Caerulomycin A

Caerulomycin A Chemical Structure

CAS No. : 21802-37-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 3 publication(s) in Google Scholar

Caerulomycin A Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Caerulomycin A is an orally active immunomodulator and antimicrobial agent. Caerulomycin A targets Smad3, STAT1 and GATA-3. Caerulomycin A downregulates GATA-3 expression, inhibits Th2 cell differentiation and Th2 cytokine production, reduces IgE levels, and alleviates pulmonary inflammatory responses and eosinophil infiltration. Caerulomycin A ameliorates collagen-induced arthritis symptoms, reduces joint inflammation and synovitis, and decreases the levels of proinflammatory cytokines in joints. Caerulomycin A inhibits the growth of some filamentous fungi, yeasts and specific bacteria. Caerulomycin A can be used in research related to arthritis and asthma[1][2][3].

IC50 & Target

Antifungal[1]
TGF-β-Smad3[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.26 μM
Compound: 7
Cytotoxicity against human A549 cells after 24 hrs by SRB assay
Cytotoxicity against human A549 cells after 24 hrs by SRB assay
[PMID: 21770434]
HL-60 IC50
0.71 μM
Compound: 7
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 21770434]
K562 IC50
> 50 μM
Compound: 7
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
[PMID: 21770434]
KB IC50
> 50 μM
Compound: 7
Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
[PMID: 21770434]
In Vitro

Caerulomycin A (0-0.31 μM; 5 days, 72 h) dose-dependently induces CD4+Foxp3+ Treg generation in non-polarizing conditions, synergistically enhances TGF-β-mediated Treg generation, suppresses Th1 and Th17 cell differentiation and cytokine secretion, reduces CD44 expression, and increases mitochondrial membrane potential in mouse naïve CD4+ T cells[1].
Caerulomycin A (0.04-0.15 μM; 48 h, 4 days) dose-dependently suppresses CD4+ effector T cell activation and alloreactive T cell proliferation in mouse cell cultures via generated Tregs (with or without TGF-β)[1].
Caerulomycin A (0.04-0.31 μM; 24 h pre-incubation) dose-dependently suppresses IFN-γ/IL-6-mediated STAT1 signaling by enhancing SOCS1 expression, reduces STAT1 target gene and protein expression, and enhances TGF-β-mediated Smad3 signaling in mouse CD4+ T cells[1].
Caerulomycin A (0.04-0.15 μM; 5 days) dose-dependently rescues mouse CD4+Foxp3+ Treg generation from IFN-γ-mediated suppression, and this Treg generation is strictly dependent on Smad3 activity[1].
Caerulomycin A (0.08-0.31 μM; 6 days) inhibits IL-4 expression in terminally differentiated mouse Th2 CD4+ T cells, with a concentration-dependent reduction in IL-4+ cell percentage over 6 days[2].
Caerulomycin A (0.08-0.31 μM; 6 days) concentration-dependently inhibits the differentiation of mouse naïve CD4+ T cells to Th2 cells, reducing both IL-4 expression (with significant inhibition at 0.31 μM) and GATA-3 expression in IL-4+ CD4+ T cells after 6 days of culture[2].
Caerulomycin A (5-100 μg/mL; up to 96 h) inhibits growth of diverse yeasts, filamentous fungi, uredospores, and bacteria in an agar dilution assay, with complete inhibition ranging from 5 μg/mL (for Candida albicans, Saccharomyces cerevisiae, Isaria cretacea, Rhizopus nigricans at 24 h) to 100 μg/mL (for Escherichia coli and Puccinia graminis var. tritici race 15B uredospore germination at all time points) when incubated at 28°C for up to 96 hours[3].
Caerulomycin A (50 μg/mL; 7-day fermentation) inhibits growth of Candida albicans in a disc diffusion assay, produced via a 7-day fermentation of Streptomyces caeruleus PRL 1687 in starch-Czapelt medium[3].

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

Caerulomycin A Related Antibodies
In Vivo

Caerulomycin A (1-10 mg/kg; daily; 50 days) dose-dependently ameliorates collagen-induced arthritis in male DBA/1 mice by expanding CD4+Foxp3+ Tregs and suppressing proinflammatory cytokines, with the 10 mg/kg daily dose yielding the greatest reduction in disease severity, inflammation, and proinflammatory mediators[1].
Caerulomycin A (1-10 mg/kg; p.o.; daily; 12 days) dose-dependently attenuates asthma symptoms in OVA-induced BALB/c mice, with the 10 mg/kg oral daily dose achieving significant suppression of lung inflammation, eosinophil infiltration, Th2 cytokine production, and IgE levels[2].

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

Animal Model: DBA/1 (male, 6-8 weeks of age, collagen-induced arthritis model)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: daily; 50 days
Result: Reduced arthritis clinical severity scores in a dose-dependent manner.
Showed significantly reduced inflammatory response and bone degeneration, with the 10 mg/kg dose showing the greatest reduction.
Significantly decreased knee joint proinflammatory cytokine levels (IFN-γ, TNF-α, IL-6).
Increased percentage of Tregs in draining lymph nodes, with the 10 mg/kg group reaching 13% CD4+Foxp3+ cells.
Significantly reduced IFN-γ and TNF-α secretion in in vitro restimulated lymph node cells with bovine collagen type II.
Significantly lowered serum levels of MMP-3.
Animal Model: BALB/c (female, 6-8 weeks old, OVA-induced asthma model)[2]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; daily; 12 days (days 13-24)
Result: Significantly reduced lung inflammation.
Reduced IL-5 and IL-13 levels in BAL fluid from.
Significantly reduced total IgE levels in BAL fluid.
Significantly reduced lung inflammation.
Significantly reduced total BAL fluid cell counts.
Molecular Weight

229.24

Formula

C12H11N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C2=NC=CC=C2)=NC(/C=N/O)=C1
Structure Classification
Initial Source

Streptomyces caeruleus
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 : 150 mg/mL (654.34 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 4.3622 mL 21.8112 mL 43.6224 mL
5 mM 0.8724 mL 4.3622 mL 8.7245 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
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Concentration
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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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Volume (start)

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C2

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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: ≥ 2.5 mg/mL (10.91 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 (10.91 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)

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
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 4.3622 mL 21.8112 mL 43.6224 mL 109.0560 mL
5 mM 0.8724 mL 4.3622 mL 8.7245 mL 21.8112 mL
10 mM 0.4362 mL 2.1811 mL 4.3622 mL 10.9056 mL
15 mM 0.2908 mL 1.4541 mL 2.9082 mL 7.2704 mL
20 mM 0.2181 mL 1.0906 mL 2.1811 mL 5.4528 mL
25 mM 0.1745 mL 0.8724 mL 1.7449 mL 4.3622 mL
30 mM 0.1454 mL 0.7270 mL 1.4541 mL 3.6352 mL
40 mM 0.1091 mL 0.5453 mL 1.0906 mL 2.7264 mL
50 mM 0.0872 mL 0.4362 mL 0.8724 mL 2.1811 mL
60 mM 0.0727 mL 0.3635 mL 0.7270 mL 1.8176 mL
80 mM 0.0545 mL 0.2726 mL 0.5453 mL 1.3632 mL
100 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0906 mL
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Caerulomycin A 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:

Caerulomycin A21802-37-9Cerulomycin CaerulomycinFungalAntibioticCandida albicansIL-6STAT1Th2 cellsTGF-βCD4+Foxp3+ TregsSmad3SOCS1GATA-3IFN-γInhibitorinhibitorinhibit

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