MCC950 - 97%, high purity , CAS No.210826-40-7, Inhibitor of NLRP3

Item Number
M414276
Grouped product items
SKUSizeAvailabilityPrice Qty
M414276-2mg
2mg
In stock
$39.90
M414276-5mg
5mg
In stock
$49.90
M414276-10mg
10mg
In stock
$84.90
M414276-50mg
50mg
In stock
$326.90
M414276-100mg
100mg
In stock
$555.90

NLRP3 Inhibitors

Basic Description

Synonyms1-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)-3-[4-(2-hydroxypropan-2-yl)furan-2-yl]sulfonylurea | N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide | CRID3 | CP-456,773 | 6RS86E2BWQ
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsMCC950 (CP-456773, CRID3) is a potent and selective inhibitor of NLRP3 (NOD-like receptor (NLR) family, pyrin domain-containing protein 3) with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of NLRP3
Product Description

Information

MCC950 MCC950 is a potent and selective inhibitor of NLRP3 with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.


Targets

NLRP3 (BMDM-based assay); NLRP3 (HMDM-based assay) 7.5 nM; 8.1 nM


In vitro

MCC950 is a potent, selective, small molecule inhibitor of NLRP3. MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. MCC950 is active in ex vivo samples from individuals with Muckle-Wells syndrome.

MCC950 reduces Interleukin-1p (IL-1β) production in vivo and attenuates the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. Furthermore, MCC950 treatment rescues neonatal lethality in a mouse model of CAPS.


Cell Research(from reference)

Cell lines:BMDM, HMDM, PBMC, HEK293T cells 

Concentrations:0.001 μM–10 μM, 5 nM–1000 nM 

Incubation Time:30 min, 45 min 

Associated Targets(Human)

NLRP3 Tchem NACHT, LRR and PYD domains-containing protein 3 (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C18 Tchem Cytochrome P450 2C18 (42 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2A6 Tchem Cytochrome P450 2A6 (2861 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
THP-1 (11052 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2J2 Tchem Cytochrome P450 2J2 (258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NLRP3 Tchem NACHT, LRR and PYD domains-containing protein 3 (908 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
J774.A1 (2436 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488196420
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488196420
IUPAC Name 1-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)-3-[4-(2-hydroxypropan-2-yl)furan-2-yl]sulfonylurea
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)
InChi Key HUUSXLKCTQDPGL-UHFFFAOYSA-N
Canonical SMILES CC(C)(C1=COC(=C1)S(=O)(=O)NC(=O)NC2=C3CCCC3=CC4=C2CCC4)O
Isomeric SMILES CC(C)(C1=COC(=C1)S(=O)(=O)NC(=O)NC2=C3CCCC3=CC4=C2CCC4)O
PubChem CID 9910393
Molecular Weight 404.48

Certificates

Certificate of Analysis(COA)

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16 results found

Lot NumberCertificate TypeDateItem
E2416333Certificate of AnalysisApr 28, 2024 M414276
E2416334Certificate of AnalysisApr 28, 2024 M414276
E2416335Certificate of AnalysisApr 28, 2024 M414276
E2416336Certificate of AnalysisApr 28, 2024 M414276
I2410220Certificate of AnalysisApr 28, 2024 M414276
D2422048Certificate of AnalysisApr 26, 2023 M414276
E23301359Certificate of AnalysisApr 26, 2023 M414276
E23301362Certificate of AnalysisApr 26, 2023 M414276
E23301375Certificate of AnalysisApr 26, 2023 M414276
E23301376Certificate of AnalysisApr 26, 2023 M414276
E23301379Certificate of AnalysisApr 26, 2023 M414276
E23301380Certificate of AnalysisApr 26, 2023 M414276
E23301381Certificate of AnalysisApr 26, 2023 M414276
E23301384Certificate of AnalysisApr 26, 2023 M414276
E23301387Certificate of AnalysisApr 26, 2023 M414276
E23301401Certificate of AnalysisApr 26, 2023 M414276

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 81 mg/mL (200.25 mM); Ethanol: 3 mg/mL (7.41 mM); Water: Insoluble;

Related Documents

Citations of This Product

1. De-Wen Bi, Ying-Xin Zhao, Xiong Qiu, Xue-Cong Zhang, Ya-Ling Zhou, Muhammad Aurang Zeb, Wen-Hui Pang, Rui Li, Meng-Ru Wang, Bin Cheng, Jing-Jing Zhang, Xing-Jie Zhang, Xiao-Li Li, Rui-Han Zhang, Wei-Lie Xiao.  (2022)  Callicarpanes A–L, Twelve New Clerodane Diterpenoids with NLRP3 Inflammasome Inhibitory Activity from Callicarpa integerrima.  CHEMISTRY & BIODIVERSITY,  20  (1): (e202200985).  [PMID:36433761] [10.1002/cbdv.202200985]

References

1. Tate MD, Ong JDH, Dowling JK, McAuley JL, Robertson AB, Latz E, Drummond GR, Cooper MA, Hertzog PJ, Mansell A.  (2016)  Reassessing the role of the NLRP3 inflammasome during pathogenic influenza A virus infection via temporal inhibition..  Sci Rep,  (13): (27912).  [PMID:27283237] [10.1021/op500134e]
2. Coll RC, Robertson AA, Chae JJ, Higgins SC, Muñoz-Planillo R, Inserra MC, Vetter I, Dungan LS, Monks BG, Stutz A et al..  (2015)  A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases..  Nat Med,  21  (3): (248-55).  [PMID:25686105] [10.1021/op500134e]
3. Coates BM, Staricha KL, Ravindran N, Koch CM, Cheng Y, Davis JM, Shumaker DK, Ridge KM.  (2017)  Inhibition of the NOD-Like Receptor Protein 3 Inflammasome Is Protective in Juvenile Influenza A Virus Infection..  Front Immunol,  (13): (782).  [PMID:28740490] [10.1021/op500134e]
4. Hettwer J, Hinterdobler J, Miritsch B, Deutsch MA, Li X, Mauersberger C, Moggio A, Braster Q, Gram H, Robertson AAB et al..  (2021)  Interleukin-1β suppression dampens inflammatory leukocyte production and uptake in atherosclerosis..  Cardiovasc Res,  71  (13): (1755-70).  [PMID:34718444] [10.1093/cvr/cvab337]
5. Ni B, Pei W, Qu Y, Zhang R, Chu X, Wang Y, Huang X, You H.  (2021)  MCC950, the NLRP3 Inhibitor, Protects against Cartilage Degradation in a Mouse Model of Osteoarthritis..  Oxid Med Cell Longev,  2021  (13): (4139048).  [PMID:34777685] [10.1021/op500134e]
6. Kennedy CR, Goya Grocin A, Kovačič T, Singh R, Ward JA, Shenoy AR, Tate EW.  (2021)  A Probe for NLRP3 Inflammasome Inhibitor MCC950 Identifies Carbonic Anhydrase 2 as a Novel Target..  ACS Chem Biol,  16  (6): (982-990).  [PMID:34003636] [10.1021/op500134e]
7. Corcoran SE, Halai R, Cooper MA.  (2021)  Pharmacological Inhibition of the Nod-Like Receptor Family Pyrin Domain Containing 3 Inflammasome with MCC950..  Pharmacol Rev,  73  (3): (968-1000).  [PMID:34117094] [10.1021/op500134e]
8. Zeng W, Wu D, Sun Y, Suo Y, Yu Q, Zeng M, Gao Q, Yu B, Jiang X, Wang Y.  (2021)  The selective NLRP3 inhibitor MCC950 hinders atherosclerosis development by attenuating inflammation and pyroptosis in macrophages..  Sci Rep,  11  (1): (19305).  [PMID:34588488] [10.1021/op500134e]
9. Wang S, Yuan YH, Chen NH, Wang HB.  (2019)  The mechanisms of NLRP3 inflammasome/pyroptosis activation and their role in Parkinson's disease..  Int Immunopharmacol,  67  (13): (458-464).  [PMID:30594776] [10.1021/op500134e]
10. Coll RC, Hill JR, Day CJ, Zamoshnikova A, Boucher D, Massey NL, Chitty JL, Fraser JA, Jennings MP, Robertson AAB et al..  (2019)  MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition..  Nat Chem Biol,  15  (6): (556-559).  [PMID:31086327] [10.1021/op500134e]
11. Ising C, Venegas C, Zhang S, Scheiblich H, Schmidt SV, Vieira-Saecker A, Schwartz S, Albasset S, McManus RM, Tejera D et al..  (2019)  NLRP3 inflammasome activation drives tau pathology..  Nature,  575  (7784): (669-673).  [PMID:31748742] [10.1021/op500134e]
12. Dekker C, Mattes H, Wright M, Boettcher A, Hinniger A, Hughes N, Kapps-Fouthier S, Eder J, Erbel P, Stiefl N et al..  (2021)  Crystal Structure of NLRP3 NACHT Domain With an Inhibitor Defines Mechanism of Inflammasome Inhibition..  J Mol Biol,  433  (24): (167309).  [PMID:34687713] [10.1021/op500134e]
13. Wang Z, Zhang S, Xiao Y, Zhang W, Wu S, Qin T, Yue Y, Qian W, Li L.  (2020)  NLRP3 Inflammasome and Inflammatory Diseases..  Oxid Med Cell Longev,  2020  (13): (4063562).  [PMID:32148650] [10.1021/op500134e]
14. Fenini G, Contassot E, French LE.  (2017)  Potential of IL-1, IL-18 and Inflammasome Inhibition for the Treatment of Inflammatory Skin Diseases..  Front Pharmacol,  (13): (278).  [PMID:28588486] [10.1021/op500134e]
15. De-Wen Bi, Ying-Xin Zhao, Xiong Qiu, Xue-Cong Zhang, Ya-Ling Zhou, Muhammad Aurang Zeb, Wen-Hui Pang, Rui Li, Meng-Ru Wang, Bin Cheng, Jing-Jing Zhang, Xing-Jie Zhang, Xiao-Li Li, Rui-Han Zhang, Wei-Lie Xiao.  (2022)  Callicarpanes A–L, Twelve New Clerodane Diterpenoids with NLRP3 Inflammasome Inhibitory Activity from Callicarpa integerrima.  CHEMISTRY & BIODIVERSITY,  20  (1): (e202200985).  [PMID:36433761] [10.1002/cbdv.202200985]

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