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Cat.No.S7809
| Related Targets | PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX |
|---|---|
| Other NLRP3 Inhibitors | MCC950 CY-09 INF39 NLRP3 Inflammasome Inhibitor I Dapansutrile YQ128 NT-0796 BMS-986299 BAL-0028 AZD4144 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| mouse BMDM cells | Function assay | 30 mins | Inhibition of NLRP3 in mouse BMDM cells preincubated for 30 mins followed by ATP addition by ELISA analysis. IC50=0.0075 μM | 26422006 | ||
| mouse BMDM cells | Function assay | 30 mins | Inhibition of NLRP3 inflammasome activation in LPS-stimulated mouse BMDM assessed as reduction in NLRP3 inflammasome-induced IL-1beta production preincubated for 30 mins followed by NLRP3 stimulation with ATP by ELISA. IC50=0.0075 μM | 27994733 | ||
| INS-1 cells | Function assay | 0.01 μM | 1 h | MCC950 inhibited not only inflammasome activation but also Ang II-induced IL-1β elevation and cell apoptosis in INS-1 cells. | 30939192 | |
| 16HBE cells | Cell viability assay | 0.01, 0.1, 1, 10, 100 μM | 24, 48, 72h | 100μM MCC950 functionally alleviated silica-induced activation of NLRP3 inflammasome in 16 HBE cells. | 29258746 | |
| THP-1 monocytes | Function assay | 1 μM | 30 mins | Pretreatment of THP‐1 monocytes for 30 min with this compound resulted in a significant reduction in IL‐1β release, but not pyroptosis upon transfection with LPS. | 26173988 | |
| macrophages | Function assay | 30 mins | Inhibition of NLRP3 in human monocyte derived macrophages assessed as reduction in LPS-induced IL-1beta production incubated for 30 mins followed by nigericin sodium salt stimulation for 2 hrs post LPS challenge for 3 hrs by ELISA, IC50 = 0.005 μM. | 29338910 | ||
| macrophages | Function assay | Inhibition of NLRP3 in human monocyte derived macrophages assessed as reduction in LPS-induced IL-1beta production by ELISA, IC50 = 0.008 μM. | 29338910 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
Water : 43 mg/mL Ethanol : 43 mg/mL
DMSO
: Insoluble
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In vivo |
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| Molecular Weight | 426.46 | Formula | C20H23N2O5S.Na |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 256373-96-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | CP-456773 Sodium, CRID3 Sodium | Smiles | CC(C)(C1=COC(=C1)S(=O)(=O)[N-]C(=O)NC2=C3CCCC3=CC4=C2CCC4)O.[Na+] | ||
| Targets/IC50/Ki |
NLRP3
(in BMDM (bone marrow derived macrophages)) 7.5nM
NLRP3
(in HMDM) 8.1 nM
|
|---|---|
| In vitro |
MCC950 inhibits canonical and noncanonical NLRP3 activation in BMDM and HMDM cells at IC50 of 7.5 and 8.1nM. MCC950 specifically inhibits activation of NLRP3 but not 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. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | NLRP3 / Casp-1 / BMI1 / ALDH1 / CD44 |
|
28865486 |
| Growth inhibition assay | Cell viability |
|
27670879 |
| Immunofluorescence | ALDH1 / BIM1 / CD44 |
|
28865486 |
| ELISA | IL-1β |
|
28726778 |
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