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MCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3). The corresponding IC50 values in BMDMs and HMDMs were 7.5 nM and 8.1 nM, respectively.
Brand: BCM
Target: NOD
Signaling Pathways: Immunology/Inflammation; NF-κB
In Vitro: MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. The effect of MCC950 on NLRP3 inflammasome activation is tested in mouse bone marrow derived macrophages (BMDM) and human monocyte derived macrophages (HMDM). The IC50 of MCC950 in BMDM is approximately 7.5 nM, while in HMDM it has a similar inhibitory capacity (IC50=8.1 nM). MCC950 also dose dependently inhibit IL-1β but not TNF-α secretion.MCC950 specifically blocks caspase-11-directed NLRP3 activation and IL-1β secretion upon stimulation of the non-canonical pathway. NLRC4-stimulated IL-1β and TNF-α secretion (as activated by Salmonella typhimurium) are not inhibited by MCC950 even at a concentration of 10 μM. MCC950 does not inhibit caspase-1 activation or IL-1β processing in response to S. typhimurium. The expression of pro-caspase-1 and pro-IL-1β in cell lysates is not substantially affected by MCC950 treatment.
Melting Point: 239 °C
pKa: 4.74±0.10(Predicted)
Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.
Isomeric SMILES: CC(C)(C1=COC(=C1)S(=O)(=O)NC(=O)NC2=C3CCCC3=CC4=C2CCC4)O
InChIKey: HUUSXLKCTQDPGL-UHFFFAOYSA-N
InChI: InChI=1S/C20H24N2O5S/c1-20(2,24)14-10-17(27-11-14)28(25,26)22-19(23)21-18-15-7-3-5-12(15)9-13-6-4-8-16(13)18/h9-11,24H,3-8H2,1-2H3,(H2,21,22,23)
Attribute [Chem Name] 1-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)-3-[4-(2-hydroxypropan-2-yl)furan-2-yl]sulfonylurea [Synonym] MCC950; CP-456773; CRID3 [CAS No.] 210826-40-7 [EINECS] 604-604-1 [MDL No.] MFCD28900720 [Formula] C20H24N2O5S [Molecular] 404.48 [Form] White solid [Storage] Sealed in dry. Room Temperature
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