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首页-小分子抑制剂&激动剂-Immunology/Inflammation-Interleukin Receptor-hIL-1β antagonist Compound (S)-2
hIL-1β antagonist Compound (S)-2

Chemical Structure : hIL-1β antagonist Compound (S)-2

CAS No.:

hIL-1β antagonist Compound (S)-2 (Compound (S)-2)

货号: PC-21192Not For Human Use, Lab Use Only.

Compound (S)-2 is a specific antagonist of the hIL-1β /IL-1R1 (human interleukin-1β/IL-1R1) interaction with IC50 of 4.0 uM in TR-FRET assays, binds hIL-1β with SPR Kd of 1.1 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Compound (S)-2 is a specific antagonist of the hIL-1β /IL-1R1 (human interleukin-1β/IL-1R1) interaction with IC50 of 4.0 uM in TR-FRET assays, binds hIL-1β with SPR Kd of 1.1 uM.
Compound (S)-2 efficiently inhibits reporter activity induced by hIL-1β in a reporter gene assay in HEK293 cells (IC50=5.3 uM), but not hIL-1α.
Compound (S)-2 also shows no inhibitory activity against IL-36γ using a NanoBiT reporter system.
Compound (S)-2 blocks IL-1R-mediated signaling in cells, block IL-6 release with an IC50 in the single digit micromolar rang (IC50=7.9 uM).

物理化学性质&存储条件

分子量 469.45
分子式 C26H19N3O6
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

(S)-4'-hydroxy-3'-(6-methyl-2-oxo-3-(1H-pyrazol-4-yl)indolin-3-yl)-[1,1'-biphenyl]-2,4-dicarboxylic acid

参考文献

1. Ulrich Hommel, et al. Nat Commun. 2023 Sep 7;14(1):5497.

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