For research use only. Not for therapeutic Use.
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].
NLRP3/AIM2-IN-3 (0-100 μM) displays remarkable inhibitory activity against NLRP3-and AIM2-but not NLRC4-dependent activation of caspase-1 and the release of IL-1b in human THP-1 macrophages[1].
NLRP3/AIM2-IN-3 shows inhibition of IL-1b secretion by human THP-1 macrophages, with IC50 of 0.098 μM, which is nearly 150-fold and 500-fold more potent than that of J774A.1 (14.62 μM) and bone marrow-derived macrophages (BMDMs) (48.98 μM), respectively[1].
NLRP3/AIM2-IN-3 has almost no inhibitory effect on the AIM2 inflammasome-dependent activation of caspase-1 and release of IL-1b in J774A.1 cells[1].
Catalog Number | I045193 |
CAS Number | 1787787-60-3 |
Synonyms | N-(3-hydroxyphenyl)-2-(1H-indol-6-yl)acetamide |
Molecular Formula | C16H14N2O2 |
Purity | ≥95% |
InChI | InChI=1S/C16H14N2O2/c19-14-3-1-2-13(10-14)18-16(20)9-11-4-5-12-6-7-17-15(12)8-11/h1-8,10,17,19H,9H2,(H,18,20) |
InChIKey | UOBOMCZZCHPHBU-UHFFFAOYSA-N |
SMILES | C1=CC(=CC(=C1)O)NC(=O)CC2=CC3=C(C=C2)C=CN3 |
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. |