NOD1/2 antagonist-1
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX).
For research use only. We do not sell to patients.
- CAS No.: 2704623-69-6
- Formula: C32H28ClF5N4O4
- Molecular Weight:663.03
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NOD1 1.13 μM (IC50) |
NOD2 0.77 μM (IC50) |
NOD1/2 antagonist-1 (compound 36b) (0-10 μM, 3 h) inhibits C12-iE-DAP-induced or MDP-induced NF-κB activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) suppresses inflammation via NOD1 and NOD2 activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) consistently and dose-dependently reduces the transcription of IL-6, TNF-α and IL-8, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-Blue hNOD1 and HEK-Blue hNOD2 cells[1]
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:3 h
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Result:Inhibited C12-iE-DAP-induced or MDP-induced NF-κB activation, and had no or little effect on cell growth.
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Cell Line:THP-1 cells[1]
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Concentration:1, 10 μM
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Incubation Time:1 h
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Result:Prevented the increases in p-RIP2, p-IKKα/β, p-p65, p-p38, and p-JNK and the degradation of IκBα in a dose-dependent manner, and blocked NOD1-and NOD2-mediated inflammatory cytokine secretion in THP-1 cells.
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Cell Line:THP-1 cells[1]
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Concentration:1, 10 μM
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Incubation Time:1 h
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Result:Consistently and dose-dependently reduced the transcription of IL-6, TNF-α and IL-8 stimulated by C12-iE-DAP or MDP, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6-8 weeks old, male, B16 tumor-bearing model, 4 groups, n = 7 each group)[1]
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Dosage:50 mg/kg (36b), 50 mg/kg (36b) + 12 mg/kg (PTX) (formulated in DMSO/Cremophor EL/saline at 5:5:90(v:v:v))
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Administration:IV, once every other day (36b), once every 4 days (PTX), for 16 days
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Result:Significantly reduced tumor growth compared with PTX treatment alone, and the tumor weight inhibitory rate increased from 64.07% to 85.46%.
Chemical Information
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CAS No. 2704623-69-6
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Molecular Weight 663.03
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Formula C32H28ClF5N4O4
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SMILES
O=C(C1=C(C=C2C(N(C=NC2=C1)CC(N3CCCC(F)(C3)F)=O)=O)C4=CC(Cl)=CC=C4)NCCCOC5=CC=C(C=C5)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NOD1/2 antagonist-1 Related Classifications
HY-146034 Related Classifications
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