Anti-inflammatory agent 129
Anti-inflammatory agent 129 is an orally active KDM6A/B inhibitor with EC50 = 0.37 μM. Anti-inflammatory agent 129 elevates intracellular H3K27me3 protein levels by inhibiting the demethylase activity of KDM6A/B, and downregulates LPS-induced transcription of the pro-inflammatory genes IL-1b, IL-6, and TNF-α in macrophages, reducing the number of M1-type inflammatory macrophages. Anti-inflammatory agent 129 attenuates weight loss and promotes recovery, protects colonic structure, and reduces disease activity in a DSS-induced mouse colitis model. Anti-inflammatory agent 129 can be used for research on inflammatory bowel disease.
For research use only. We do not sell to patients.
- CAS No.: 3104903-17-2
- Formula: C29H35N5O2
- Molecular Weight:485.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
KDM6 0.37 μM (EC50) |
IL-6 |
IL-8 |
TNF-α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | EC50 |
0.37 μM
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Increase of H3K27me3 levels in RAW264.7 murine macrophage cells assessed by ELISA after 24 hrs exposure.
Increase of H3K27me3 levels in RAW264.7 murine macrophage cells assessed by ELISA after 24 hrs exposure.
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42858568 |
| RAW264.7 | CC50 |
9.35 μM
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Cytotoxicity against RAW264.7 murine macrophage cells assessed as viability reduction by CCK-8 assay after 24 hrs exposure.
Cytotoxicity against RAW264.7 murine macrophage cells assessed as viability reduction by CCK-8 assay after 24 hrs exposure.
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42858568 |
In Vitro
Anti-inflammatory agent 129 (0.625-10 μM; 24 h) increases H3K27me3 levels in RAW264.7 cells in a concentration-dependent manner, confirming that it inhibits intracellular KDM6A/B[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 murine macrophage cells
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Concentration:10, 5, 2.5, 1.25, 0.625 μM
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Incubation Time:24 h
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Result:Increased H3K27me3 levels in RAW264.7 cells in a concentration-dependent manner.
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Cell Line:LPS-stimulated RAW264.7 M1 macrophages
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Concentration:10 μM
100 ng/mL (LPS) -
Incubation Time:15 h
24 h (LPS) -
Result:Reduced LPS-induced Il1b, Il6, and Tnfa expression in RAW264.7 M1 macrophages.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male; 10 weeks; 25 g; were given 2.5% (w/v) DSS in drinking water to induce experimental colitis for 6 days, followed by 6 days of regular water)
[1] -
Dosage:4 mg/kg
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Administration:i.p.; every other day; from day 0 until day 12
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Result:Attenuated body‑weight loss (-11.87 %) in experimental colitis mice.
Reduced disease‑activity‑index scores for colitic animals.
Preserved colon length in colitis‑model mice.
Maintained crypt architecture and lowered immune‑cell infiltration according to H&E staining.
Decreased the proportion of splenic CD86+ inflammatory macrophages via flow‑cytometry analysis.
Diminished the density of colonic CD86+ F4/80+ M1‑like macrophages based on multiplex immunofluorescence.
Chemical Information
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CAS No. 3104903-17-2
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Molecular Weight 485.62
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Formula C29H35N5O2
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SMILES
O=C(OCC)CCCCNC1=NC(C2=CC=CC=N2)=NC(N3CCC4(C(C=CC=C5)=C5CC4)CC3)=C1
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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)
Anti-inflammatory agent 129 Related Classifications
HY-190472 Related Classifications
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