NLRP3/AIM2-IN-3_product_DataBase

Bioactivity

NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization[1].

Invitro

NLRP3/AIM2-IN-3 (0-100 μM) 对 NLRP3 和 AIM2 表现出显着的抑制活性，但对人 THP-1 巨噬细胞中 caspase-1 的 NLRC4 依赖性激活和 IL-1b 的释放没有显着抑制作用[1]。NLRP3/AIM2-IN-3 抑制人 THP-1 巨噬细胞分泌 IL-1b，IC50 为 0.098 μM，比 NLRP3/AIM2-IN-3 强近 150 倍和 500 倍分别为 J774A.1 (14.62 μM) 和骨髓来源的巨噬细胞 (BMDM) (48.98 μM)[1]。NLRP3/AIM2-IN-3 对 J774A.1 细胞中 AIM2 炎性体依赖性 caspase-1 激活和 IL-1b 释放几乎没有抑制作用[1]。

Name

NLRP3/AIM2-IN-3

CAS

1787787-60-3

Formula

C16H14N2O2

Molar Mass

266.29

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Jiao Y, et al. Discovery of a novel and potent inhibitor with differential species-specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. Eur J Med Chem. 2022 Feb 11;232:114194.

PeptideDB

NLRP3/AIM2-IN-3

CAS: 1787787-60-3 F: C16H14N2O2 W: 266.29