MR2938

MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research[1].

Signaling Pathways >> GPCR/G Protein >> CCR

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related

Signaling Pathways >> Immunology/Inflammation >> NO Synthase

Signaling Pathways >> Immunology/Inflammation >> CCR

Signaling Pathways >> Immunology/Inflammation >> NOD-like Receptor (NLR)

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> MAPK/ERK Pathway >> JNK

Signaling Pathways >> Neuronal Signaling >> AChE

AChE:5.04 ± 0.7 μM (IC50)

BChE:>20 μM (IC50)

NF-κB

IL-1β

IL-6

NLRP3

JNK

MR2938 (0-10 μM, 24 h) 在 1.25 μM 时降低促炎细胞因子 IL-1β、TNF-α、IL-6 和 CCL2 的 mRNA 水平[1]。 MR2938 (10 μM, 24 h) 阻断 LPS 诱导的 BV-2 细胞中的 NF-κB 信号通路[1]。 MR2938 (20 μM) 对 AChE 和 BChE 具有抑制活性，抑制率分别为 91.8 ± 2.68% 和 38.7 ± 11.7%[1]。 MR2938 (0-10 μM) 对 BV2 细胞系的细胞活力影响很小[1]。 RT-PCR[1] Cell Line: BV-2 cells Concentration: 0, 1.25, 2.5, 5, and 10 μM Incubation Time: 24 h Result: Dramatically and dose dependently reduced the mRNA levels of inflammatory factors stimulated by LPS (1 μg/mL). Compared with TNF-α, the inhibitory effect of MR2938 on IL-1β, IL-6 and CCL2 was much potent. Western Blot Analysis[1] Cell Line: BV-2 cells Concentration: 10 μM Incubation Time: 24 h Result: Suppressed the expression level of p65 protein, and reduced the p-p65 level. Reduced NLRP3 expression obviously. Reduced the phosphorylation level of JNK induced by LPS stimulation, while the level of JNK protein was hardly changed.

[1]. Lv L, et al. Discovery of quinazolin-4(3H)-one derivatives as novel AChE inhibitors with anti-inflammatory activities. Eur J Med Chem. 2023 Apr 6;254:115346.