| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
NF-κB 1.58 μM (EC50)
NF-κB activator 2 targets the NF-κB pathway by promoting the phosphorylation and degradation of IκB (inhibitor of NF-κB) proteins, allowing NF-κB dimers (typically p50/p65) to translocate to the nucleus and activate target gene transcription; it may also directly activate upstream kinases such as IKK. |
|---|---|
| ln Vitro |
In SH-SY5Y neuroblastoma cells, NF-κΒ activator 2 (compound 61) (1 μM, 6 h) stimulates SOD2 mRNA expression[1].
In vitro, NF-κB activator 2 induces NF-κB activation in various cell lines as measured by NF-κB luciferase reporter assays; it upregulates the expression of NF-κB target genes including IL-6, TNF-α, and ICAM-1; it enhances inflammatory responses and immune cell activation. |
| ln Vivo |
In mice, NF-κB activator 2 (1 mg/kg; iv) has an appropriate half-life of 0.96 hours[1]. Comparable half-lives (2.86 hours), oral bioavailability (15.6%), and Cmaxes (92 ng/mL) are shown by NF-κΒ activator 2 (5 mg/kg; po)[1].
In vivo, NF-κB activator 2 has been used to study the role of NF-κB in immune responses and inflammation; it can potentiate immune responses in models of infection or vaccination; its effects are context-dependent and may vary by tissue and disease model. |
| Enzyme Assay |
Non-cellular binding assay: The activity of NF-κB activator 2 is assessed using biochemical assays for IKK kinase activity or by measuring IκBα phosphorylation and degradation in vitro using recombinant proteins; the compound is incubated with IKK and IκBα substrate, and phosphorylation is detected by Western blot or by using a kinase activity kit.
|
| Cell Assay |
Cellular assays: Cells (e.g., HEK293, HeLa, or macrophages) are transfected with an NF-κB luciferase reporter plasmid; treated with NF-κB activator 2; luciferase activity is measured to quantify pathway activation; expression of NF-κB target genes is assessed by qRT-PCR or ELISA; NF-κB nuclear translocation is visualized by immunofluorescence; cell viability is assessed by MTT assay.
|
| Animal Protocol |
In vivo animal experiments: NF-κB activator 2 is administered to mice via intraperitoneal or intravenous injection; NF-κB activation in tissues is assessed by measuring target gene expression or by using NF-κB reporter mice; immune responses are evaluated in models of infection, inflammation, or vaccination; inflammatory cytokine levels in serum and tissues are measured by ELISA.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties: NF-κB activator 2 is a small molecule with moderate oral bioavailability; it is rapidly absorbed and distributed to various tissues; it is metabolized by hepatic enzymes and has a relatively short plasma half-life; pharmacokinetic properties may vary depending on the specific compound structure.
|
| Toxicity/Toxicokinetics |
Toxicological profile: NF-κB activator 2 is a research compound with limited toxicological data; excessive NF-κB activation can lead to chronic inflammation and tissue damage; the compound should be handled with caution; standard safety precautions for research chemicals apply.
|
| References | |
| Additional Infomation |
Other information: NF-κB activator 2 is used as a research tool to study the role of NF-κB in immune regulation, inflammation, and cancer; it is not approved for clinical use; it may be used in combination with other modulators to dissect NF-κB signaling pathways.
|
| Molecular Formula |
C16H11FN2O3
|
|---|---|
| Molecular Weight |
298.27
|
| Exact Mass |
298.075
|
| CAS # |
2375281-44-8
|
| PubChem CID |
139434520
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.5
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
22
|
| Complexity |
396
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(O)(=O)C1=CC=CC(C2OC(NC3=CC=CC=C3F)=NC=2)=C1
|
| InChi Key |
VGJMPWREFUKMAD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H11FN2O3/c17-12-6-1-2-7-13(12)19-16-18-9-14(22-16)10-4-3-5-11(8-10)15(20)21/h1-9H,(H,18,19)(H,20,21)
|
| Chemical Name |
3-[2-(2-fluoroanilino)-1,3-oxazol-5-yl]benzoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO :~250 mg/mL (~838.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3527 mL | 16.7633 mL | 33.5267 mL | |
| 5 mM | 0.6705 mL | 3.3527 mL | 6.7053 mL | |
| 10 mM | 0.3353 mL | 1.6763 mL | 3.3527 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
