3104903-17-2
Chemical Structure
Anti-inflammatory agent 129
- CAS No.: 3104903-17-2
- Formula:C29H35N5O2
- Molecular Weight:485.62
InChIKey: CGFZAHRIHLMMAG-UHFFFAOYSA-N
SMILES: O=C(OCC)CCCCNC1=NC(C2=CC=CC=N2)=NC(N3CCC4(C(C=CC=C5)=C5CC4)CC3)=C1
Biological Activity: 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[1].
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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. | |||||||||||||||||||||
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