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MCC950 sodium

Catalog No. T6887 CAS 256373-96-3

Synonyms: MCC950, CP-456773 sodium, CP-456773, CRID3 sodium salt

MCC950 sodium salt (IC50 of 7.5 uM in BMDMs) is an effective, selective NLRP3 inhibitor.

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MCC950 sodium, CAS 256373-96-3

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Purity: 98%

Biological Description

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Description	MCC950 sodium salt (IC50 of 7.5 uM in BMDMs) is an effective, selective NLRP3 inhibitor.
Targets&IC50	NLRP3:7.5nM
In vitro	MCC950 specifically inhibits NLRP3 activation,canonical NLRP3 activation in BMDM IC50 is of 7.5 ,and noncanonical NLRP3 activation in HMDM cells IC50 is of 8.1 nM. MCC950 cannot inhibit activation of the AIM2, NLRC4 or NLRP1 inflammasomes.
In vivo	MCC950 reduces interleukin-1β (IL-1β) production and attenuates the severity of experimental autoimmune encephalomyelitis (EAE). Furthermore, MCC950 treatment rescues neonatal lethality in a mouse model of CAPS and is active in ex vivo samples from individuals with Muckle-Wells syndrome. [1]
Kinase Assay	kinase activity assays: All assays are carried out in 384-well white microtiter plates. Compounds are 4-fold serially diluted in 8 steps, starting from 10 μM. The reaction mixture consisted of 25 μL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contains 2.0 μg/mL FLT3 enzyme, 5 μM of poly(Glu,Tyr) substrate and 4 μM of ATP. For JAK1 assays, the reaction contains 2.5 μg/mL of JAK1 enzyme, 10 μM of poly(Glu,Ala,Tyr) substrate and 1.0 μM of ATP. For JAK2 assays, the reaction contained 0.35 μg/mL of JAK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. For JAK3 assays, the reaction contained 3.5 μg/mL of JAK3 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 6.0 μM of ATP. For TYK2 assays, the reaction contained 2.5 μg/mL of TYK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 μL PKLight? detection reagent. After 10 min incubation luminescent signals are read on a multi-label plate reader.
Cell Research	MCC950 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. BMDM are seeded at 5×105/mL or 1×106/mL, HMDM at 5×105/mL and PBMC at 2×106/mL or 5×106/mL in 96 well plates. The following day the overnight medium is replaced and cells are stimulated with 10 ng/mL LPS from Escherichia coli serotype EH100 (ra) TLRgrad for 3 h. Medium is removed and replaced with serum free medium (SFM) containing DMSO (1:1,000), MCC950 (0.001-10 μM), glyburide (200 μM), Parthenolide (10 μM) or Bayer cysteinyl leukotriene receptor antagonist 1-(5-carboxy-2{3-[4-(3-cyclohexylpropoxy)phenyl]propoxy}benzoyl)piperidine-4-carboxylic acid (40 μM) for 30 min. Cells are then stimulated with inflammasome activators: 5 mM adenosine 5'-triphosphate disodium salt hydrate (ATP) (1 h), 1 μg/mL Poly(deoxyadenylic-thymidylic) acid sodium salt (Poly dA:dT) transfected with Lipofectamine 200 (3-4 h), 200 μg/mL MSU (overnight) and 10 μM nigericin (1 h) or S. typhimurium UK-1 strain. Cells are also stimulated with 25 μg/mL Polyadenylic-polyuridylic acid (4 h). For non-canonical inflammasome activation cells are primed with 100 ng/mL Pam3CSK4 for 4 h, medium is removed and replaced with SFM containing DMSO or MCC950 and 2 μg/mL LPS is transfected using 0.25% FuGENE for 16 h. Supernatants are removed and analysed using ELISA kits. LDH release is measured using the CytoTox96 non-radioactive cytotoxicity assay[1].
Animal Research	C57BL/6 mice were injected intraperitoneally with 50 mg/kg MCC950.

Synonyms	MCC950, CP-456773 sodium, CP-456773, CRID3 sodium salt
Molecular Weight	426.46
Formula	C20H23N2NaO5S
CAS No.	256373-96-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 42.7 mg/mL (100 mM)

DMSO: 42.7 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Coll RC, et al. Nat Med. 2015, 21(3):248-55.

Related compound libraries

This product is contained In the following compound libraries：

HIF-1 Signaling Pathway Compound Library Inhibitor Library Immunology/Inflammation Compound Library NF-κB Signaling Compound Library Nonsteroidal Anti-Inflammatory Compound Library CNS-Penetrant Compound Library Bioactive Compound Library

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Related compounds with same targets

Emlenoflast Asymmetric dimethylarginine 6-Biopterin NLRP3-IN-10 L-Canavanine sulfate CY-09 MCC950 Imperatorin

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Keywords

MCC950 sodium 256373-96-3 NF-Kb信号通路免疫与炎症 NOD NOD-like Receptor (NLR) CP 456773 MCC-950 sodium MCC-950 inhibit MCC950 Inhibitor CP456773 CP-456773 CP-456773 sodium CRID3 CRID 3 MCC 950 CRID3 sodium salt CRID-3 inhibitor

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