MyD88 degrader-1
MyD88 degrader-1 is an orally active molecular glue degrader targeting MyD88, with a DC50 of 0.74 μM, and exhibits potent anti-inflammatory activity. MyD88 degrader-1 promotes ubiquitination and proteasomal degradation of MyD88, blocks the activation of the NF-κB signaling pathway, and downregulates the transcription of pro-inflammatory genes such as IL-6 and IL-1β. MyD88 degrader-1 alleviates symptoms in acute lung injury models. MyD88 degrader-1 can be used in studies related to acute lung injury.
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- 화학식: C23H22N6O6S
- 분자량:510.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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NF-κB |
IL-6 |
IL-1β |
MyD88 degrader-1 (compound d21) potently inhibits LPS-induced IL-6 secretion in J774A.1 mouse macrophages, with an IC50 of 0.42 μM; it also potently suppresses LPS-induced IL-6 secretion in human monocytic THP-1 cells (IC50 = 0.097 μM) and mouse macrophage RAW cells (IC50 = 0.56 μM)[1].
MyD88 degrader-1 (0.125-1 μM; 2 h pretreatment, followed by 6 h LPS stimulation) dose-dependently inhibits LPS-induced transcription of the IL-6 gene in J774A.1 mouse macrophages[1].
MyD88 degrader-1 (0.01-1 μM) induces dose-dependent degradation of MyD88 protein in J774A.1 mouse macrophages, with a DC50 of 0.74 μM[1].
MyD88 degrader-1 (10 μM; 2 h pretreatment followed by 30 min LPS stimulation) inhibits LPS-induced activation of the NF-κB pathway in J774A.1 mouse macrophages by maintaining IκBα levels and reducing p65 nuclear translocation[1].
MyD88 degrader-1 directly binds to and stabilizes MyD88 and RNF126 proteins in J774A.1 mouse macrophages, and promotes the formation of a ternary complex between MyD88 and RNF126 in J774A.1 mouse macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J774A.1 mouse macrophage cells
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Concentration:0.125, 0.25, 0.5, 1 μM
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Incubation Time:0.5 h pretreatment, followed by 24 h LPS stimulation
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Result:Inhibited 94.55% of LPS-induced IL-6 secretion at 1 μM.
Exhibited an IC50 of 0.42 μM for IL-6 secretion inhibition.
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Cell Line:J774A.1 mouse macrophage cells
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Concentration:0.125, 0.25, 0.5, 1 μM
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Incubation Time:2 h pretreatment, followed by 6 h LPS stimulation
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Result:Inhibited LPS-induced IL-6 gene transcription in a dose-dependent manner.
Caused significant inhibition at all tested concentrations.
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Cell Line:J774A.1 mouse macrophage cells
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Concentration:1 μM
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Incubation Time:2 h treatment; 1 h MG132 pretreatment before MyD88 degrader-1; 15 min LPS stimulation after pretreatment
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Result:Significantly reduced MyD88 protein levels when used alone.
Had its degradation effect abrogated by cotreatment with MG132.
Markedly decreased MyD88 abundance under LPS stimulation.
Had its LPS-stimulated MyD88 reduction effect reversed by MG132 (HY-13259).
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Cell Line:J774A.1 mouse macrophage cells
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Concentration:10 μM
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Incubation Time:2 h pretreatment, followed by 30 min LPS stimulation
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Result:Inhibited LPS-induced NF-κB pathway activation in J774A.1 mouse macrophage cells by preserving IκBα levels and reducing p65 nuclear translocation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 18-22 g, CLP-induced sepsis model)[1]
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Dosage:20 mg/kg
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Administration:p.o.; single dose; 30 minutes pre-surgery
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Result:Reduced CLP group relative lung wet/dry weight ratio, BALF total cell number, BALF and serum IL-6, serum IL-1β, CLP-triggered splenomegaly, and CLP-caused alveolar pathological lesions plus alveolar leukocyte recruitment.
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Animal Model:C57BL/6 (male, 18-22 g, LPS-induced model)[1]
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Dosage:20 mg/kg
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Administration:p.o.; single dose; 30 minutes pre-LPS challenge
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Result:Reduced lung wet/dry weight ratio, BALF total cell count and total protein, systemic and pulmonary IL-6, LPS-triggered splenomegaly, alveolar pathological lesions and alveolar leukocyte infiltration simultaneously.
Chemical Information
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분자량 510.52
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화학식 C23H22N6O6S
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SMILES
NC1=CC=NN1S(=O)(C2=CC=C(C([N+]([O-])=O)=C2)N3CCN(C(/C=C/C(C4=CC=CC=C4)=O)=O)CC3)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MyD88 degrader-1 Related Classifications
HY-184470 Related Classifications
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