SMU-H1
SMU-H1 is a TLR2 agonist with a KD of 12.1 nM for mouse TLR2 and an EC50 of 5.14 nM in HEK-Blue hTLR2 cells. SMU-H1 binds TLR2 and activates MyD88-dependent signaling. SMU-H1 activates the NF-κB and MAPK signaling pathways. SMU-H1 induces proinflammatory cytokine production. SMU-H1 promotes M1 macrophage polarization and dendritic cell activation. SMU-H1 can be used for research on Lewis lung cancer.
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- CAS. Nr.: 2410782-67-9
- Formel: C18H16F3N3O3S
- Molecular Weight:411.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
TLR2 12.1 nM (Kd) |
TLR2 5.14 nM (EC50) |
NF-κB |
MyD88 |
p38 MAPK |
IKKα |
IKKβ |
p65 |
p38 |
JNK1 |
JNK2 |
ERK1 |
ERK2 |
IL-6 |
IL-1β |
In Vitro
SMU-H1 (6.25-100 μM) directly binds recombinant mouse TLR2 with a KD of 12.1 nM in SPR[1].
SMU-H1 (0.001-10 μM; 24 h) is a specific TLR2 agonist with an EC50 of 5.14 nM in HEK-Blue hTLR2 cells[1].
SMU-H1 (0.02-100 μM; 24-72 h) shows detectable cytotoxicity against HEK-Blue hTLR2 and RAW 264.7 cells only at 100 μM, while exhibiting no obvious cytotoxicity against LLC cells[1].
SMU-H1 (5-10 μM; 15-30 min) activates NF-κB and MAPK signaling in wild-type peritoneal macrophages in a TLR2-dependent manner[1].
SMU-H1 (24 h) promotes M1-like macrophage polarization and dendritic cell activation through the TLR2 signaling pathway[1].
SMU-H1 (0.01-10 μM; 24 h) induces TNF-α, IL-6, and IL-1β production in RAW 264.7, THP-1, and mouse peritoneal macrophages in a dose-dependent and TLR2-dependent manner[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, RAW 264.7 cells, and LLC cells
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Concentration:0.02 μM; 0.05 μM; 0.14 μM; 0.41 μM; 1.23 μM; 3.70 μM; 11.11 μM; 33.33 μM; 100 μM
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Incubation Time:24, 48, 72 h
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Result:Exerted detectable cytotoxic effects on HEK-Blue hTLR2 cells and RAW 264.7 cells only at a high concentration of 100 μM, and no obvious cytotoxic effect was observed in LLC cells.
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Cell Line:Wild-type peritoneal macrophages
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Concentration:5 μM; 10 μM
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Incubation Time:15 min; 30 min
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Result:Significantly induced the phosphorylation of IKKα/β, p65, p38, JNK1/2 and ERK1/2. Reduced the expression of phosphorylated IκBα.
Parmacokinetics
In Vivo
SMU-H1 (10 mg/kg; intraperitoneal injection; once every 2 days; days 14-26) inhibits LLC tumor growth in C57BL/6 mice, reduces excised tumor weight, and promotes intratumoral immune cell infiltration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks)[1]
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Dosage:SMU-H1 10 mg/kg
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Administration:i.p.; every 2 days; days 14-26
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Result:The vehicle group showed accelerated tumor growth, resulting in markedly larger tumor volume and heavier tumor weight than the SMU-H1- and 5-FU-treated groups.
The vehicle group exhibited heavier tumor weight than the SMU-H1-treated group.
Frequencies of total lymphocytes, NK cells, DCs, and M1-like macrophages within tumor tissue were significantly increased by SMU-H1.
Compared with the vehicle group, the SMU-H1 group had markedly higher proportions of CD4+ T cells and CD8+ T cells within tumor-infiltrating lymphocytes.
The numbers of NK cells, DCs, and M1-like macrophages in tumors were also proportionally elevated.
No significant differences in body weight were observed between the vehicle group and SMU-H1- and 5-FU-treated groups.
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Animal Model:C57BL/6 (male, 6−8 weeks)[1]
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Dosage:SMU-H1 10 mg/kg combined with 5-FU 5 mg/kg
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Administration:i.p.; every 2 days; days 14-26
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Result:Combined administration of 5-FU and SMU-H1 exerted stronger antitumor efficacy than either alone, leading to further reduction in tumor volume.
In the same LLC efficacy study, excised tumors were dissected and weighed on day 27, and the vehicle group exhibited markedly heavier tumor weight than the combination-treated group.
Chemical Information
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CAS. Nr. 2410782-67-9
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Molecular Weight 411.40
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Formel C18H16F3N3O3S
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SMILES
O=S(C1=CC=C(NC)C(N2C=C(C3=CC=C(C(F)(F)F)C=C3O)N=C2)=C1)(C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SMU-H1 Related Classifications
HY-189658 Related Classifications
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Keywords
- SMU-H1
- 2410782-67-9
- Toll-like Receptor (TLR)
- MyD88
- NF-κB
- p38 MAPK
- IKK
- ERK
- JNK
- Interleukin Related
- Lewis lung carcinoma
- M1-like macrophage polarization
- MAPK signaling pathways
- MyD88-dependent signaling
- TLR2
- antitumor immune responses
- dendritic cell activation
- lymphocyte infiltration
- pro-inflammatory cytokine production
- Inhibitor
- inhibitor
- inhibit