2. Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. Toll-like Receptor (TLR) NF-κB p38 MAPK
  4. SMU-R39

SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.

For research use only. We do not sell to patients.

SMU-R39

SMU-R39 Chemical Structure

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SMU-R39 Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Description

SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis[1].

IC50 & Target[1]

TLR7

2.36 μM (Kd)

TLR8

105 nM (Kd)

TLR7

3.22 μM (IC50)

TLR8

0.24 μM (IC50)

In Vitro

SMU-R39 (0.1-30 μM, 24 h) shows potent inhibitory activity against R848-induced SEAP signal in HEK-Blue hTLR8 cells (IC50 = 0.24 μM) and moderate inhibitory activity in HEK-Blue hTLR7 cells (IC50 = 3.22 μM)[1].
SMU-R39 (0.01-10 μM, 24 h) strongly blocks Resiquimod (R848) (HY-13740)-induced SEAP signal elevation in THP1-Dual cells with an IC50 of 0.18 μM, demonstrating its ability to inhibit NF-κB activation via TLR7/8 signaling[1].
SMU-R39 (0.046-100 μM, 24 h) dose-dependently inhibited R848-activated TLR7/8 activation in HEK-Blue hTLR7/8 and THP1-Dual cells SMU-R39 (5-10 μM, 0.5 h) downregulates the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages, suppressing TLR7/8 downstream NF-κB and MAPK signaling pathways[1].
SMU-R39 (0.1-20 μM, 24 h) significantly reduces TNF-α secretion in R848-stimulated THP-1 macrophages, Raw 264.7 cells, and PBMCs in a concentration-dependent manner[1].
SMU-R39 (0.1-20 μM, 6 h) effectively decreases the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1].

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

SMU-R39 Related Antibodies

Real Time qPCR[1]

Cell Line: R848-stimulated THP-1 macrophages and PBMCs
Concentration: 0.1, 1, 10, 20 μM
Incubation Time: 6 h
Result: Decreased the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1].

Western Blot Analysis[1]

Cell Line: R848-stimulated THP-1 macrophages
Concentration: 5, 10 μM
Incubation Time: 0.5 h
Result: Downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages [1].
In Vivo

SMU-R39 (0.5%-1.0% ointment, topical, once daily, 7 days) significantly alleviates Imiquimod (IMQ) (HY-B0180)-induced psoriatic skin inflammation in female BALB/c mice[1].

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

Animal Model: IMQ-induced psoriasis mouse model: 5% Imiquimod (IMQ) ointment (62.5 mg) was topically applied to the hairless dorsal skin of 8-12-week-old female BALB/c mice once daily for 7 consecutive days[1]
Dosage: 0.5%, 1.0% ointment
Administration: topical, once daily, 7 days
Result: Achieved a psoriasis area and severity index (PASI) reduction.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Downregulated the gene expression of skin TNF-α, IFN-α , IL-17 , IL-22 , and IL-23 .
Achieved an epidermal thickness reduction.
Molecular Weight

387.48

Formula

C23H25N5O
SMILES

OC1=CC=C(N2C=NC3=C2C4=CC=CC=C4N=C3N5CCN(CC)CC5)C=C1C
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-R39 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-R39Toll-like Receptor (TLR)NF-κBp38 MAPKNuclear factor-κBNuclear factor-kappaBpsoriasisTLR7TLR8MAPKPBMCsTHP-1 cellsInhibitorinhibitorinhibit

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