| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 500mg | |||
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| Other Sizes |
| Targets |
SUN24595 specifically targets the NF-κB signaling pathway, functioning as a potent activator of NF-κB with an EC50 of 0.9 μM. NF-κB is a family of transcription factors (including p50, p52, RelA/p65, RelB, and c-Rel) that regulate the expression of hundreds of genes involved in immune responses, inflammation, cell survival, proliferation, and differentiation. In resting cells, NF-κB is sequestered in the cytoplasm by inhibitory IκB proteins. Activation of NF-κB involves phosphorylation and degradation of IκB proteins, allowing NF-κB to translocate to the nucleus and activate target gene transcription. SUN24595 induces NF-κB activation, leading to the expression of NF-κB target genes including superoxide dismutase (SOD) 2. SOD2 is a mitochondrial antioxidant enzyme that plays a critical role in protecting cells from oxidative stress.
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| ln Vitro |
In vitro, SUN24595 potently activates NF-κB with an EC50 of 0.9 μM. The compound induces NF-κB activation in cell-based reporter assays, leading to the transcription of NF-κB target genes. One of the genes induced by SUN24595 is superoxide dismutase (SOD) 2, a mitochondrial antioxidant enzyme. SOD2 induction suggests that SUN24595 may modulate cellular redox balance and protect cells from oxidative stress. The compound's ability to activate NF-κB makes it a valuable tool for studying the role of NF-κB in various cellular processes, including inflammation, immunity, and cell survival. Specific details of the compound's in vitro activity are described in the primary literature.
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| ln Vivo |
In vivo activity of SUN24595 has been investigated in preclinical models. As a potent NF-κB activator, the compound is expected to modulate NF-κB-dependent gene expression in vivo, affecting immune responses, inflammation, and other physiological processes. By inducing SOD2 expression, SUN24595 may also influence oxidative stress responses in vivo. Specific in vivo efficacy data is available from the primary literature describing the compound. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage in these studies.
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| Enzyme Assay |
NF-κB activation by SUN24595 is typically assessed using cell-based reporter gene assays. Cells are transfected with a luciferase reporter construct containing NF-κB response elements (κB sites) upstream of a minimal promoter. Cells are treated with varying concentrations of the compound, and luciferase activity is measured to quantify NF-κB transcriptional activation. EC50 values are calculated from dose-response curves. NF-κB activation can also be confirmed by measuring the phosphorylation and degradation of IκB proteins by Western blotting, and by assessing NF-κB nuclear translocation using immunofluorescence. Target gene expression (including SOD2) is quantified by qRT-PCR.
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| Cell Assay |
Cellular assays for SUN24595 are performed using cell lines suitable for NF-κB studies, such as HEK293, HeLa, or macrophage cell lines. Cells are treated with varying concentrations of the compound for specified time periods. NF-κB activation is assessed using reporter gene assays as described above. IκBα degradation and NF-κB p65 phosphorylation and nuclear translocation are assessed by Western blotting and immunofluorescence. SOD2 mRNA and protein levels are measured by qRT-PCR and Western blotting. Cell viability and proliferation are assessed using standard assays to evaluate the functional consequences of NF-κB activation.
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| Animal Protocol |
In vivo studies of SUN24595 are conducted in rodent models of inflammation, immunity, or other conditions where NF-κB plays a role. The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage. Tissues are collected for analysis of NF-κB target gene expression by qRT-PCR. SOD2 expression and activity are assessed in various tissues. Inflammatory markers and immune cell activation are evaluated. Pharmacodynamic markers of NF-κB activation are assessed to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SUN24595 (molecular weight 314.33, molecular formula C16H11FN2O2S) have been characterized. The compound is available as a light yellow to yellow solid powder with ≥98% purity. Storage recommendations include appropriate conditions for research chemicals. Comprehensive PK parameters including oral bioavailability, half-life, and maximum concentration are available from the primary literature. The compound's molecular properties, including its fluorine-containing structure, may influence its pharmacokinetic and distribution characteristics.
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| Toxicity/Toxicokinetics |
SUN24595 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have been conducted as part of preclinical development. NF-κB is a master regulator of inflammation and immunity, and its activation may have diverse biological effects that would be carefully evaluated in toxicology studies. Standard safety pharmacology assessments would include evaluation of effects on immune function, inflammation, and cell survival.
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| References | |
| Additional Infomation |
SUN24595 is a research-grade compound used as a pharmacological tool for studying NF-κB signaling pathways. NF-κB is a family of transcription factors that plays a central role in regulating immune responses, inflammation, cell survival, and proliferation. The compound is also known as NF-κB activator 1 and was first reported in the European Journal of Medicinal Chemistry (2021, 210, 112952). SUN24595 activates NF-κB with an EC50 of 0.9 μM and induces superoxide dismutase (SOD) 2 mRNA expression. The compound is available with ≥98% purity for research use. SUN24595 serves as a valuable tool for studying the role of NF-κB in inflammation, immunity, and cancer, and for validating NF-κB as a therapeutic target.
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| Molecular Formula |
C16H11FN2O2S
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|---|---|
| Molecular Weight |
314.334145784378
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| Exact Mass |
314.05
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| Elemental Analysis |
C, 61.14; H, 3.53; F, 6.04; N, 8.91; O, 10.18; S, 10.20
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| CAS # |
2387524-59-4
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| PubChem CID |
151901137
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
398
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C=C(C2C=CC=C(C(=O)O)C=2)N=C1NC1C=CC=CC=1F
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| InChi Key |
SSUFECODNVILSX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11FN2O2S/c17-12-6-1-2-7-13(12)18-16-19-14(9-22-16)10-4-3-5-11(8-10)15(20)21/h1-9H,(H,18,19)(H,20,21)
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| Chemical Name |
3-(2-((2-fluorophenyl)amino)thiazol-4-yl)benzoic acid
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| Synonyms |
NF-κΒ activator 1; SUN24595; SUN-24595; SUN 24595;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~397.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.62 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (6.62 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1814 mL | 15.9068 mL | 31.8137 mL | |
| 5 mM | 0.6363 mL | 3.1814 mL | 6.3627 mL | |
| 10 mM | 0.3181 mL | 1.5907 mL | 3.1814 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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