SMU-Z1
Based on 1 Customer Validation
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.
- Purity : 99.42%
- CAS No.: 2410782-66-8
- Formula: C17H13F3N4O3
- Molecular Weight:378.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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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.
In Vivo
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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CAS No. 2410782-66-8
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Appearance Solid
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Molecular Weight 378.31
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Formula C17H13F3N4O3
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Color Light yellow to yellow
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (264.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.61 mM); Suspended solution; Need warming and heat to 60°C
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Monocyte-derived dendritic cell differentiation
Human monocyte-derived dendritic cells are generated by isolating PBMC-derived monocytes and culturing them with GM-CSF plus IL-4, which produces cells with dendritic-cell antigen-presenting properties, reduced monocyte phenotype, and increased dendritic-cell functional readouts such as antigen uptake, allogeneic T-cell stimulation, and expression of markers including HLA-DR, CD80, CD86, CD83, CD1a, or CD209 depending on protocol and maturation state. The main readout is phenotypic and functional differentiation: immature MoDCs are commonly evaluated by loss or reduction of CD14 with acquisition of dendritic-cell markers and antigen uptake capacity, whereas mature MoDCs are evaluated by increased CD83, CD80, CD86, HLA-DR, and T-cell stimulatory function after exposure to maturation stimuli such as TNF-α or a cytokine/PGE2 cocktail.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6433 mL | 13.2167 mL | 26.4333 mL | 66.0834 mL |
| 5 mM | 0.5287 mL | 2.6433 mL | 5.2867 mL | 13.2167 mL | |
| 10 mM | 0.2643 mL | 1.3217 mL | 2.6433 mL | 6.6083 mL | |
| 15 mM | 0.1762 mL | 0.8811 mL | 1.7622 mL | 4.4056 mL | |
| 20 mM | 0.1322 mL | 0.6608 mL | 1.3217 mL | 3.3042 mL | |
| 25 mM | 0.1057 mL | 0.5287 mL | 1.0573 mL | 2.6433 mL | |
| 30 mM | 0.0881 mL | 0.4406 mL | 0.8811 mL | 2.2028 mL | |
| 40 mM | 0.0661 mL | 0.3304 mL | 0.6608 mL | 1.6521 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5287 mL | 1.3217 mL | |
| 60 mM | 0.0441 mL | 0.2203 mL | 0.4406 mL | 1.1014 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8260 mL | |
| 100 mM | 0.0264 mL | 0.1322 mL | 0.2643 mL | 0.6608 mL |
SMU-Z1 Related Classifications
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