SMU-Z1
SMU-Z1 is a TLR1/2 heterodimer agonist with an EC50 of 4.88 nM. SMU-Z1 activates the NF-κB pathway, triggers pro-inflammatory cytokine production, and induces the generation of TNF-α, IL-1β, IL-6 and NO. SMU-Z1 promotes splenocyte proliferation and upregulates the expression of CD8+T cells, NK cells and dendritic cells. SMU-Z1 exhibits significant anti-tumor effects in mouse leukemia models. SMU-Z1 can be used for leukemia-related research.
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- No. CAS: 2410782-66-8
- Fòrmula: C17H13F3N4O3
- Peso molecular:378.31
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Almacenamiento:
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Actividad biológica
SMU-Z1 specifically activates the TLR1/2 heterodimer in HEK-Blue hTLR2 cells, with an EC50 of 4.88 × 10-9 M[1].
SMU-Z1 (0-10 μM; 24 h) dose-dependently stabilizes the TLR2 protein in HEK-Blue hTLR2 cells[1].
SMU-Z1 (0-5 μM; 24 h) dose-dependently activates the NF-κB signaling pathway in stably transfected human macrophage U937 cells[1].
SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in Raw 264.7 mouse macrophages[1].
SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in human peripheral blood mononuclear cells (PBMC)[1].
SMU-Z1 (0-1000 nM; 24 h) stimulates Raw 264.7 mouse macrophages to produce NO[1].
SMU-Z1 (0-10 μM; 24 h) upregulates the mRNA expression of IL-6 and IL-8 in PBMC[1].
SMU-Z1 (0-5 μM; 24-72 h) promotes the proliferation of primary splenocytes from C57Bl/6 mice[1].
SMU-Z1 (0-1000 nM; 48-72 h) dose-dependently activates the proliferation of naive T cells isolated from C57Bl/6 mice[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
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Concentration:0, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Increased TLR2 protein stability in a dose-dependent manner, with higher TLR2 protein levels observed as concentrations increased from 0.01 to 10 μM.
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Cell Line:Raw 264.7 mouse leukemic monocyte macrophage cells
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Concentration:0.0007, 0.002, 0.006, 0.018, 0.036, 0.12, 0.4, 1 μM (TNF-α); 0.0015, 0.0043, 0.0133, 0.04, 0.12, 0.4, 1.2, 3.6, 10 μM (IL-1β)
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Incubation Time:24 h
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Result:Stimulated dose-dependent production of TNF-α and IL-1β.
Increased TNF-α levels from ~2000 pg/mL at 0.006 μM to ~4000 pg/mL at 1 μM.
Increased IL-1β levels from ~50 pg/mL at 0.0043 μM to ~550 pg/mL at 10 μM.
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Cell Line:C57Bl/6 mouse primary splenocytes
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Concentration:0, 0.1, 0.5, 1, 5 μM
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Incubation Time:0, 24, 48, 72 h
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Result:Dependently promoted proliferation of C57Bl/6 mouse primary splenocytes, with a 3-5-fold increase observed at 5 μM after 48 h of incubation.
SMU-Z1 (0.1 mg; intraperitoneal injection; single dose) increases the frequencies of splenic CD8+ T cells and CD3+CD8+TLR2+ T cells in normal mice[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 (8-week-old male, 17-19 g, subcutaneous inoculation of 5 × 105 syngeneic murine FBL3 leukemia cancer cells)[1]
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Dosage:0.3 mg
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Administration:i.p.; once every 5 days
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Result:Reduced mean tumor volume to 386 mm3 on day 35 (vs. 2370 mm3 in PBS controls).
Induced complete tumor disappearance in 3 out of 7 treated mice after three administrations.
Increased splenic CD3+ T cells to 25.7% (vs. 11.6% in controls).
Increased splenic CD8+ T cells to 19.4% (vs. 10.6% in controls).
Increased splenic CD8/CD4 ratio to 0.28 (vs. 0.13 in controls).
Increased splenic NK cells to 10.5% (vs. 4.64% in controls).
Increased splenic DC cells to 3.87% (vs. 1.54% in controls).
Increased tumor tissue CD3+ T cells to 37.0%.
Increased tumor tissue CD8+CD3+ T cells to 28.1%.
Increased tumor tissue NK cells to 3.66%.
Increased tumor tissue DC cells to 4.12%.
Caused no significant change in mouse body weight relative to controls.
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Animal Model:C57BL/6 (8-10-week-old male)[1]
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Dosage:0.1 mg
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Administration:i.p.; single administration
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Result:Increased splenic CD8+ T cells to 27.4% after 7 days (vs. 17.1% in PBS controls).
Increased splenic CD8+ T cells to 21.3% after 5 days (vs. 16.7% in PBS controls).
Increased splenic CD3+CD8+TLR2+ T cells to 6.3% after 5 days (vs. 2.6% in PBS controls).
Increased splenic CD3+CD8+TLR2+ T cells to 6.7% after 7 days (vs. 2.6% in PBS controls).
Reduced splenic CD4+ T cells to 55.6% (vs. 69.5% in PBS controls).
Increased the splenic CD8/CD4 ratio.
Caused no significant change in splenic CD19+ B cell frequencies.
Chemical Information
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No. CAS 2410782-66-8
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Peso molecular 378.31
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Fòrmula C17H13F3N4O3
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SMILES
CNC(C(N1C=NC(C2=C(O)C=C(C(F)(F)F)C=C2)=C1)=C3)=CC=C3[N+]([O-])=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SMU-Z1 Related Classifications
HY-182644 Related Classifications
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