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Chemical Structure : PU.1 inhibitor A11
CAS No.: 873588-27-3
Catalog No.: PC-21942Not For Human Use, Lab Use Only.
PU.1 inhibitor A11 is a small molecule inhibitor of transcription factor PU.1 with EC50 of 2.5 nM in reporter assays, moderates the inflammatory response in human iPSC-derived microglia-like cells (iMGLs) by downregulating inflammatory PU.1-target gene expression without affecting hematopoiesis.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $118 | In stock | |
| 50 mg | $168 | In stock | |
| 100 mg | $248 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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PU.1 inhibitor A11 is a small molecule inhibitor of transcription factor PU.1 with EC50 of 2.5 nM in reporter assays, moderates the inflammatory response in human iPSC-derived microglia-like cells (iMGLs) by downregulating inflammatory PU.1-target gene expression without affecting hematopoiesis.
A11 is a potent inhibitor of Zymosan A bioparticle and myelin uptake in iMGLs (EC50 < 35 nM), moderates microglial activation in iMGLs.
A11 reduces PU.1-dependent expression by enabling MECP2-dependent repression at PU.1 motifs.
A11 reduces neuropathology and improves cognitive performance in mouse models of Alzheimer's disease (AD)-related neurodegeneration, tauopathy, and β-amyloid deposition, without affecting peripheral hematopoiesis or causing other side effects.
A11 stimulates the recruitment of MECP2, HDAC1, and other co-repressor molecules to PU.1 target genes, such as IL1B and CD14, without affecting PU.1 expression levels.
A11 represents a first-in-class molecule of drugs that converts PU.1 from a transcriptional activator to a transcriptional repressor, resulting in a controlled state of microglial inflammation.
| M.Wt | 330.45 | |
| Formula | C18H22N2O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-cyclohexyl-N-(pyridin-4-ylmethyl)benzenesulfonamide |
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1. Ralvenius WT, et al. J Exp Med. 2023 Nov 6;220(11):e20222105.
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