PU.1 inhibitor A11

Chemical Structure : PU.1 inhibitor A11

CAS No.: 873588-27-3

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货号: PC-21942Not For Human Use, Lab Use Only.

规格	价格	库存
25 mg	￥1180	In stock
50 mg	￥1680	In stock
100 mg	￥2480	In stock
200 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	330.45
分子式	C18H22N2O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-cyclohexyl-N-(pyridin-4-ylmethyl)benzenesulfonamide

参考文献

1. Ralvenius WT, et al. J Exp Med. 2023 Nov 6;220(11):e20222105.