ENDO12
ENDO12 is an inhibitor of the Munc13-4-STX7 protein complex, with a Kd value of 2.7 µM for STX7. ENDO12 blocks the interaction of Munc13-4-STX7. ENDO12 inhibits endolysosomal flux, endolysosomal cargo degradation, the extracellular signal-regulated kinase signaling pathway in neutrophils, the IFN regulatory factor signaling pathway in plasmacytoid dendritic cells, and the responses of primary dendritic cells to TLR3, TLR7, and TLR9. ENDO12 alleviates CpG-induced systemic inflammation by reducing the levels of myeloperoxidase, IL-6 and IFNγ. ENDO12 does not interfere with the host's antiviral response to lymphocytic choriomeningitis virus infection.\nENDO12 can be used in studies related to systemic inflammation.
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- Fòrmula: C15H17FN4O
- Peso molecular:288.32
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Almacenamiento:
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
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IL-6 |
TLR3 |
TLR9 |
TLR7 |
In Vitro
ENDO12 (31.25 nM-3 μM) binds to recombinant STX7 with a Kd value of 2.7 µM, showing higher affinity than ENDO3[1].
ENDO12 potently inhibits CpG-induced TLR9 activation in HEK-Blue hTLR9 cells, with an IC50 of 1 × 10-7 M[1].
ENDO12 (10 µM; 1 h) reduces the colocalization levels of STX7 with Munc13-4, TLR7 with LAMP1, and TLR9 with LAMP1 in RAW 264.7 mouse macrophages, thereby inhibiting endosome maturation and TLR trafficking[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 murine macrophages
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Concentration:10 µM
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Incubation Time:1 h
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Result:Significantly decreased colocalization of STX7 with Munc13-4.
Significantly decreased colocalization of TLR7 and TLR9 with LAMP1+ organelles, indicating impaired endosomal maturation and TLR trafficking to late endolysosomes.
In Vivo
ENDO12 (15 mg/kg; i.p.; single dose; 1 hour before LCMV infection) does not impair the host antiviral response to LCMV infection in mice, with only minimal reduction in MIP1β and MIP2 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male and female, 6-10 weeks old)[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose; 1 hour before CpG challenge
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Result:Significantly reduced CpG-induced plasma levels of interleukin 6 (IL-6), interferon gamma (IFNγ), and myeloperoxidase (MPO) compared to vehicle-treated controls.
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Animal Model:C57BL/6J mice (male and female, 8 weeks old)[1]
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Dosage:15 mg/kg
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Administration:i.p.; single dose; 1 hour before LCMV infection
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Result:Did not significantly alter plasma levels of IL-6, IFNα, IFNγ, or MPO induced by LCMV infection.
Caused only a mild reduction in plasma levels of macrophage inflammatory proteins MIP1β and MIP2, while all other measured cytokines and chemokines remained unchanged compared to vehicle-treated controls.
Chemical Information
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Peso molecular 288.32
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Fòrmula C15H17FN4O
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SMILES
CCN(CC)C1=CC=C(/N=N/C2=NC=C(F)C=C2)C(O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ENDO12 Related Classifications
HY-183079 Related Classifications
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