2. Immunology/Inflammation NF-κB MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. Toll-like Receptor (TLR) MyD88 IKK p38 MAPK ERK TNF Receptor Interleukin Related
  4. SMU-L11-R

SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.

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SMU-L11-R

SMU-L11-R Chemical Structure

CAS No. : 3040320-18-8

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SMU-L11-R Related Antibodies

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IKK-α IKK-β IKK IKKε TBK1

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies[1].

IC50 & Target[1]

human TLR7

0.024 μM (EC50)

TLR8

2.56 μM (EC50)

In Vitro

SMU-L11-R (0-100 μM; 24 h; HEK-Blue hTLR7 cells) shows no obvious toxic effect[1].
SMU-L11-R (0-100 μM; 24 h; MC38 and B16-F10 cells) shows cytotoxic in MC38 and B16-F10 cells at a high testing concentration (100 μM)[1].
SMU-L11-R (0, 0.1, 1, 5, 10 μM; 24 h; Peritoneal macrophages) shows dose-dependent increase in M1-like macrophages[1][1].
SMU-L11-R (1 μM; 15-120 min; BMDCs) can activate TLR7 downstream signaling pathways through MyD88 protein, including the NF-κB, MAPK signaling pathways[1].
SMU-L11-R (0, 0.01, 0.1, 1, 10 μM; 24 h; HEK-Blue hTLR7 cells) shows dose-dependent increase in TLR7 protein[1].
SMU-L11-R (0-10 μM; 24 h; Raw 264.7 cells) shows significant increase in TNF-α and IL-6[1].
SMU-L11-R (0-10 μM; 24 h; human PBMCs) shows dose-dependent increase in TNF-α and IL-1β[1].
SMU-L11-R (0-10 μM; 24 h; mouse BMDCs) shows significant increase in IL-6[1].
SMU-L11-R (0, 0.1, 1, 10 μM; 24 h; peritoneal macrophages) shows concentration-dependent increase in NO production[1]. SMU-L11-R also shows the activation of TLR8 (EC50 = 2.56 μM) with the increase of concentration, but the activation was 156 times smaller than that of TLR7. SMU-L11-R induces activation of HEK-Blue hTLR2, hTLR3 or hTLR4 was negligible[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SMU-L11-R Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK-Blue hTLR7 cells
Concentration: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed no obvious toxic effect.

Cell Viability Assay[1]

Cell Line: MC38 cells
Concentration: 0.02 μM, 0.05 μM, 0.14 μM, 1.23 μM, 11.11 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed cytotoxic effect at a high testing concentration (100 μM).

Cell Viability Assay[1]

Cell Line: B16-F10 cells
Concentration: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed cytotoxic effect at a high testing concentration (100 μM).

Western Blot Analysis[1]

Cell Line: HEK-Blue hTLR7 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed dose-dependent increase in TLR7 protein.

Western Blot Analysis[1]

Cell Line: BMDCs
Concentration: 1 μM
Incubation Time: 15 min, 30 min, 60 min, 90 min, 120 min
Result: Showed significant induction of the phosphorylation of IKK α/ β, p65, p38 and ERK1/2 in BMDCs.

ELISA Assay[1]

Cell Line: Raw 264.7 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed significant increase in TNF-α and IL-6.

ELISA Assay[1]

Cell Line: Mouse BMDCs
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed significant increase in IL-6.

ELISA Assay[1]

Cell Line: Human PBMCs
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed dose-dependent increase in TNF-α and IL-1β.
In Vivo

SMU-L11-R (5-10 mg/kg; IP; every 2 days; 15 days) inhibits mouse MC38 tumor growth and enhances anti-tumor effects when combined with PD-L1 inhibitors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57/BL6 wild-type male mice (6-8 weeks old) were injected subcutaneousely with 2 x 105 MC38 cells[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: IP; every 2 days; 15 days
Result: Significantly inhibited tumor growth and exhibited excellent synergistic anti-tumor effects when combined with PD-L1 inhibitors by upregulating CD8+ T cells.
Molecular Weight

324.42

Formula

C19H24N4O
CAS No.
SMILES

NC1=NC2=CC=CC=C2C3=C1N=C(CCCC)N3C[C@@H]4COCC4
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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SMU-L11-R 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:

SMU-L11-R3040320-18-8Toll-like Receptor (TLR)MyD88IKKp38 MAPKERKTNF ReceptorInterleukin RelatedIκB kinaseI kappa B kinase Extracellular signal regulated kinasesTumor Necrosis Factor ReceptorTNFRILInflammatory cytokinesTLR7 agonistCD8(+)T cellsCancer immunotherapyPD-L1Inhibitorinhibitorinhibit

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