NIC-0102,2806031-94-5

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NIC-0102

CAS No. : 2806031-94-5

MCE 国际站：NIC-0102

产品活性：NIC-0102 是一种口服有效的蛋白酶体 (proteasome) 抑制剂 (pIC₅₀=7.55)，能特异性地抑制 NLRP3 炎症小体激活。NIC-0102 在体内对 DSS 诱导的溃疡性结肠炎模型显示出有效的抗炎作用。NIC-0102还能抑制前 IL-1β 的产生。

研究领域：Metabolic Enzyme/Protease  |  Immunology/Inflammation

作用靶点：Proteasome  |  NOD-like Receptor (NLR)

In Vitro: NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells.
NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells.
NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells.
NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells.

In Vivo: NIC-0102 (0.125, 0.25, 0.5 mg/kg; p.o.; single every 72 h for 10 days) shows strong protection against DSS-induced acute colitis in mice.

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