1. Immunology/Inflammation NF-κB Apoptosis
  2. Toll-like Receptor (TLR) NF-κB TNF Receptor Interleukin Related
  3. 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.

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

SMU-Z1

SMU-Z1 Chemical Structure

CAS No. : 2410782-66-8

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Description

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[1].

In Vitro

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.

Western Blot Analysis[1]

Cell Line: HEK-Blue hTLR2 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
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.

ELISA Assay[1]

Cell Line: Raw 264.7 mouse leukemic monocyte macrophage cells
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)
Incubation Time: 24 h
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.

Cell Proliferation Assay[1]

Cell Line: C57Bl/6 mouse primary splenocytes
Concentration: 0, 0.1, 0.5, 1, 5 μM
Incubation Time: 0, 24, 48, 72 h
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.
In Vivo

SMU-Z1 (0.3 mg; intraperitoneal injection; once every 5 days; D7-D32) reduces tumor volume in leukemia xenograft mouse models, while increasing the frequencies of CD8+ T cells, NK cells and DC cells infiltrating the spleen and tumors[1].
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.

Animal Model: C57BL/6 (8-week-old male, 17-19 g, subcutaneous inoculation of 5 × 105 syngeneic murine FBL3 leukemia cancer cells)[1]
Dosage: 0.3 mg
Administration: i.p.; once every 5 days
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.
Animal Model: C57BL/6 (8-10-week-old male)[1]
Dosage: 0.1 mg
Administration: i.p.; single administration
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.
Molecular Weight

378.31

Formula

C17H13F3N4O3

CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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SMU-Z1
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