General
Preferred name
MCC950
Synonyms
CP-456773 ()
CRID3 sodium salt ()
CP-456773 sodium ()
MCC950 sodium ()
MCC-950 ()
MCC950 (sodium) ()
CRID3 ()
CP-456773, CRID3 ()
MCC950 Sodium (CP-456773 Sodium) ()
MCC950 (sodium salt) ()
P&D ID
PD017644
CAS
256373-96-3
210826-40-7
Tags
available
probe
drug candidate
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
PRICE 67
COMMENT This probe has been tested in human primary cell-based assays (BioMAP Diversity PLUS panel from Eurofins Discovery) at 370 – 10 uM. Selectively active in only one of the 12 assay systems at 370 nM, 1.1 uM and 3.3 uM. Activity is restricted to the BioMAP LPS system, a co-culture stimulated with LPS, so consistent with the target. It was not active in a system containing differentiated macrophages stimulated through TLR2. Sep 15 2020 - 8:32am
DESCRIPTION MCC950 has been reported as a potent, selective and direct inhibitor of the NLRP3 inflammasome . The compound binds directly at a motif within the NLRP3 protein's NACHT domain and blocks its activation and inflammasome formation which ultimately reduces cleavage of IL-1β and IL-18 from their latent forms. It offers a useful tool for examination of NLRP3 biology and its potential for therapeutic intervention. MCC950 has demonstrated anti-inflammatory actions in numerous in vivo models of human diseases and has been proposed as a therapeutic option for the treatment of NLRP3-associated diseases, including IL-1β/IL-18-driven inflammatory/autoinflammatory conditions and other diseases that have an inflammatory component such as atherosclerosis , type 2 diabetes, Alzheimer's and Parkinson's diseases , cancer and pathologic inflammation that is a result of viral infection . (GtoPdb)
DESCRIPTION MCC950 (CP-456773; CRID3) is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
PRICE 67
DESCRIPTION CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1?? secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1?? production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION HSF1 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION MCC950 sodium is a potent, selective NLRP3 inhibitor. MCC950 sodium salt shows analgesic agent effect. (Enamine Bioactive Compounds)
DESCRIPTION MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1. (TargetMol Bioactive Compound Library)
DESCRIPTION CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
21
AdooQ Bioactive Compound Library
A13478
Cayman Chemical Bioactives
34762
17510
Chemical Probes.org
mcc950
Concise Guide to Pharmacology 2017/18
8228
Concise Guide to Pharmacology 2019/20
8228
Concise Guide to Pharmacology 2021/22
8228
Concise Guide to Pharmacology 2023/24
8228
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DM6J2UZ
Enamine Bioactive Compounds
EBC-07801
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101301
Guide to Pharmacology
8228
High-quality chemical probes
PD017644
MedChem Express Bioactive Compound Library
HY-12815A
HY-12815
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
mcc950-sodium-salt
mcc950
TargetMol Bioactive Compound Library
T6887
T3701
Tocris Bioactive Compound Library
5479
External IDs
36
Properties
(calculated by RDKit )
Molecular Weight
404.14
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
2
cLogP
2.99
TPSA
108.64
Fraction CSP3
0.45
Chiral centers
0.0
Largest ring
6.0
QED
0.73
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
NLRP3
NOD-like Receptor (NLR)
Primary Target
Cytokines
Member status
member
MOA
NRLP3 inflammasome inhibitor
inhibits NLRP3 inflammasome (exact target/mechanism unknown). Shows reduction of IL-1B in vivo in EAE expt models of MS.
NOD like receptor inhibitor
Pathway
Immunology/Inflammation
NF-κB
Target subclass
NACHT, LRR and PYD domains-containing Protein
Source data