2. Immunology/Inflammation
  3. Toll-like Receptor (TLR) IFNAR Interleukin Related
  4. 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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ENDO12

ENDO12 Chemical Structure

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ENDO12 Related Antibodies

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Description

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[1].

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.

ENDO12 Related Antibodies

Immunofluorescence[1]

Cell Line: RAW 264.7 murine macrophages
Concentration: 10 µM
Incubation Time: 1 h
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 (30 mg/kg; i.p.; single dose; 1 hour before CpG challenge) reduces CpG-induced systemic inflammation in mice, lowering plasma IL-6, IFNγ, and MPO levels[1].
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.

Animal Model: C57BL/6J mice (male and female, 6-10 weeks old)[1]
Dosage: 30 mg/kg
Administration: i.p.; single dose; 1 hour before CpG challenge
Result: Significantly reduced CpG-induced plasma levels of interleukin 6 (IL-6), interferon gamma (IFNγ), and myeloperoxidase (MPO) compared to vehicle-treated controls.
Animal Model: C57BL/6J mice (male and female, 8 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.p.; single dose; 1 hour before LCMV infection
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.
Molecular Weight

288.32

Formula

C15H17FN4O
SMILES

CCN(CC)C1=CC=C(/N=N/C2=NC=C(F)C=C2)C(O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ENDO12 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ENDO12ENDO 12ENDO-12Toll-like Receptor (TLR)IFNARInterleukin RelatedInterferon-α/β receptorInterferon-alpha/beta receptor ILdendritic cellsTLR9HEK-Blue hTLR9 cellsTLR7plasmacytoid dendritic cellsMunc13-4-STX7 protein complexTLR3RAW 264.7 murine macrophagesJurkat-Dual cellsneutrophilsInhibitorinhibitorinhibit

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