Anti-inflammatory agent 128
Anti-inflammatory agent 128 is a 2-azido-3-O-benzyl-2-deoxy sp2-iminosugar glycolipid with anti-inflammatory, antitumor, and antiparasitic activities. Anti-inflammatory agent 128 exhibits broad-spectrum antiproliferative activity against multiple human tumor cell lines. Anti-inflammatory agent 128 elevates mitochondrial ROS levels in Leishmania donovani promastigotes. Anti-inflammatory agent 128 inhibits the inflammatory response of Bv.2 microglia under LPS stimulation, suppresses NLRP3 inflammasome activation, downregulates the pro-inflammatory mediators Tnfa, Il1β, and Il6, and upregulates Hmox1. Anti-inflammatory agent 128 attenuates reactive gliosis in isolated retinal explants from diabetic rats and ameliorates inflammation-related phenotypes associated with diabetic retinopathy. Anti-inflammatory agent 128 can be used in research on tumors, leishmaniasis, and diabetic retinopathy.
For research use only. We do not sell to patients.
- Formula: C26H40N4O6S
- Molecular Weight:536.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NLRP3 |
IL-6 |
IL-8 |
Caspase-1 |
TNF-α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
8.5 μM
|
Antiproliferative activity against human A549 lung cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human A549 lung cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| HeLa | GI50 |
2.8 μM
|
Antiproliferative activity against human HeLa cervix cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human HeLa cervix cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| MIA PaCa-2 | GI50 |
9.2 μM
|
Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human MIA PaCa-2 pancreatic cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| SW1573 | GI50 |
8.9 μM
|
Antiproliferative activity against human SW1573 lung cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human SW1573 lung cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| T47D | GI50 |
5.4 μM
|
Antiproliferative activity against human T-47D breast cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human T-47D breast cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| WiDr | GI50 |
3.6 μM
|
Antiproliferative activity against human WiDr colon cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
Antiproliferative activity against human WiDr colon cancer cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay.
|
42828963 |
| THP-1 | IC50 |
11.66 μM
|
Inhibition of intracellular Leishmania major amastigote growth in THP-1 macrophage-differentiated cells after 72 hrs by luciferase assay.
Inhibition of intracellular Leishmania major amastigote growth in THP-1 macrophage-differentiated cells after 72 hrs by luciferase assay.
|
42828963 |
| MRC5 | CC50 |
35.11 μM
|
Cytotoxicity against human MRC-5 lung fibroblasts assessed as viability reduction after 72 hrs by resazurin assay.
Cytotoxicity against human MRC-5 lung fibroblasts assessed as viability reduction after 72 hrs by resazurin assay.
|
42828963 |
| THP-1 | CC50 |
37.98 μM
|
Cytotoxicity against human THP-1 macrophages assessed as viability reduction after 72 hrs by resazurin assay.
Cytotoxicity against human THP-1 macrophages assessed as viability reduction after 72 hrs by resazurin assay.
|
42828963 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bv.2 microglial cells
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Concentration:0.1, 0.5, 1.0, 5.0, and 10 µM
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Incubation Time:24 h
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Result:Cell survival was not compromised at any tested concentration after 24 h.
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Cell Line:Bv.2 microglial cells
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Concentration:10 µM
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Incubation Time:24 h
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Result:Attenuated LPS-induced Tnfa, Il6, and Il1b mRNA expression in Bv.2 microglia.
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Cell Line:Bv.2 microglial cells
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Concentration:10 µM
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Incubation Time:24 h
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Result:Reduced LPS-induced NLRP3 protein levels.
Chemical Information
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Molecular Weight 536.68
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Formula C26H40N4O6S
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SMILES
O=C1N2[C@H](S(=O)(CCCCCCCCCCCC)=O)[C@H](N=[N+]=[N-])C(OCC3=CC=CC=C3)[C@H](O)[C@H]2CO1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Anti-inflammatory agent 128
- Parasite
- NOD-like Receptor (NLR)
- Interleukin Related
- Caspase
- TNF Receptor
- Reactive Oxygen Species (ROS)
- HMOX1
- Leishmania
- NLRP3 inflammasome
- amastigote
- diabetic retinopathy
- heme oxygenase-1
- microglia
- pro-inflammatory cytokines
- reactive oxygen species
- retinal explants
- Inhibitor
- inhibitor
- inhibit