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NIC-0102

Catalog No.GC71149

NIC-0102 es un inhibidor de proteosoma activo por vía oral (pIC50=7.55) que inhiespecíficamente la activación de la vesícula inflamnlrp3.

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NIC-0102 Chemical Structure

Cas No.: 2806031-94-5

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
242,00 $
Disponible
1 mg
104,00 $
Disponible
5 mg
263,00 $
Disponible
10 mg
446,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.

NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells[1].
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[1].
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[1].
NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells[1].

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[1].

References:
[1]. Wu X, et al. Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. J Med Chem. 2022 Sep 5.

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