SMU-C409
SMU-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research.
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- CAS No.: 3113739-61-7
- Formule: C21H21N3OS2
- Masse moléculaire:395.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
SMU-C409 (0-100 nM) selectively activates the hTLR2 signaling pathway in HEK-Blue hTLR2 cells while showing negligible activity on other TLR subtypes (hTLR3/4/7/8)[1].
SMU-C409 (0-100 μM, 24 h) shows low toxicity in HEK-Blue hTLR2 cells, PBMC, B16−F10 cells and MCF-7 cells[1].
SMU-C409 (0-50 μM, 0-24 h) specifically targets and activates TLR2 in HEK-Blue hTLR2 and THP-1 cells[1].
SMU-C409 (0-100 μM, 0-700 min) binds hTLR2 protein with the Kd of 72.4 nM[1].
SMU-C409 (0-20 μM, 0-120 min) activates the TLR1/2 hetero dimer, triggering downstream signaling via MyD88 recruit ment, which promotes phosphorylation of MyD88-NF-κB pathway components and dissociation of inhibitory proteins in THP-1(Phorbol 12-myristate 13-acetate (HY-18739) PMA differentiated) cells[1].
SMU-C409 (0.01-10 μM, 24 h) plays a pivotal role in inflammatory signaling by stimulating downstream cytokine production through the NF-κB pathway and maintains conserved species specificity across different immune cell types and signaling axes in THP-1 cells (PMA-differentiated), PBMC cells, mouse peritoneal macrophages and mouse RAW264.7 cells[1].
SMU-C409 (0-10 μM, 48 h) exhibits a degree of immune activating activity in CD3 + cells, CD4 + cells, CD8 + cells, Monocytes, B cells and NK cells[1].
SMU-C409 (1-20 μM, 24 h) enhances immune cell mediated induction of SJSA-1 apoptosis, showing the potential for antitumor immune activity[1].
SMU-C409 (8 h) exhibits markedly improved plasma stability with degradation rate constant (k) of 0.0003 min -1 in rat plasma[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 hTLR2 cells, PBMC, B16−F10 cells and MCF-7 cells
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Concentration:0, 0.14, 0.41, 1.23, 3.7, 11.11, 33.3 and 100 μM
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Incubation Time:24 h
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Result:Showed no obvious toxicity to HEK-BluehTLR2 cells, peripheral blood mononuclear cells (PBMC), B16−F10 cells or MCF-7 cells at a high concentration of 100 μM.
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Cell Line:HEK-Blue TLR2 cells or THP-1 cells
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Concentration:0, 0.01, 0.1, 1, 10, or 50 μM
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Incubation Time:0, 15, 30, 60, 90, or 120 min
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Result:Showed SMU-C409 dose dependently upregulated TLR2 expression in both HEK-Blue hTLR2 cells and PMA-differentiated THP-1 cells.
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Cell Line:Wild-type THP-1 cells and TLR2 knockdown THP-1 cells
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Concentration:20, 40 μM
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Incubation Time:24 h
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Result:Induced TNF-α in wild-type cells but not inTLR2-knockdown cells.
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Cell Line:THP-1(PMA differentiated) cells
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Concentration:0, 10 and 20 μM
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Incubation Time:0, 15, 30, 60, 90, 120 min and 24 h
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Result:Upregulated TLR1 and TLR2 protein expression after 24 h stimulation at 20 μM.
Induced time-dependent phos phorylation of IKKα/β, p65, and p38 (evident by 15 min, with peak dynamics varying by protein) and progressive IκBα dissociation in THP-1 cells, coupled with subsequent IκBα recovery by 120 min.
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Cell Line:THP-1 cells (PMA-differentiated), PBMC cells, mouse peritoneal macrophages and mouse RAW264.7 cells.
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Concentration:0, 0.01, 0.1, 1, 5 and 10 μM
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Incubation Time:24 h
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Result:Induced dose dependent secretion of TNF-α and IL-1β in both freshly isolated human PBMCs and PMA-differentiated THP-1 cells.
Showed no significant effect on TNF-α and IL-6 secretion in murine peritoneal macrophages.
Failed to elicit concentration-dependent NO activation in mouse RAW264.7 cells.
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Cell Line:SJSA-1 (GFP labeled), Jurkat T cells, and PMA-differentiated THP-1 cells
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Concentration:0, 0.01, 0.1, 1, 5 and 10 μM
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Incubation Time:24 h
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Result:Resulted the spontaneous apoptosis rate (4.91%) of SJSA-1 cells.
Resulted an increase apoptosis rate from 7.69 to 13.77%. in SJSA-1 cells cocultured with Jurkat T and PMA-differentiated THP-1 cells.
Chemical Information
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CAS No. 3113739-61-7
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Masse moléculaire 395.54
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Formule C21H21N3OS2
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SMILES
CC(C)C(C1=C(NC(NC2=C3C=CC=NC3=CC=C2)=S)SC4=C1CCC4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SMU-C409 Related Classifications
HY-180580 Related Classifications
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