All AbMole products are for research use only, cannot be used for human consumption.
IQ-1S is also a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. The effect of IQ-1S is evaluated on LPS-induced cytokine production in human PBMCs. Among the 12 cytokines analyzed, LPS (200 ng/mL) consistently induces five (IL-1α, IL-1β, IL-6, IL-10, and TNF-α) in PBMCs compared with DMSO-treated control cells. Production of all of these cytokines is significantly inhibited by 20 μM IQ-1S. Among them, TNF-α production is inhibited completely by IQ-1 (>99%), the levels of IL-1α, IL-1β, and IL-10 are decreased by 85%, and IL-6 production is decreased by 33%.
In vivo, when mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1) i.p., the serum exposure of the compound is also good, with AUC0-12h values of 2.9 and 7.4 μM/h, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | Human PBMCs |
| Preparation method | Human PBMCs are plated in 96-well plates at a density of 2×105 cells/well in culture medium supplemented with 3% (v/v) endotoxin-free FBS. PBMCs are pretreated with 20 μM IQ-1 or DMSO for 30 min, followed by addition of 200 ng/ml LPS for 24 h. A human cytokine MultiAnalyte ELISArray Kit is used to evaluate various cytokines (IL-1α, IL-1β, IL-2, IL-4, IL-6, IL-8, IL-10, IL-12, IL-17A, interferon (IFN)-γ, TNF-α, and granulocyte-macrophage colony-stimulating factor in supernatants of PBMCs. |
| Concentrations | 20 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c mice |
| Formulation | |
| Dosages | 12.5 or 30 mg/kg |
| Administration | i.p. |
| Molecular Weight | 247.25 |
| Formula | C15H9N3O |
| CAS Number | 23146-22-7 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related JNK Products |
|---|
| JIP-1(153-163)
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide). |
| JNK3 inhibitor-5
JNK3 inhibitor-5 is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. |
| JNK-1-IN-1
JNK-1-IN-1 is a JNK-1 inhibitor. |
| JNK2-IN-1
JNK2-IN-1 is a JNK2 inhibitor (Kds: 79.2 μM). |
| JNK-1-IN-2
JNK-1-IN-2 is a JNK-1 inhibitor (IC50: 33.5 nM). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
