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IQ-1S

Cat. No. M8946
IQ-1S Structure
Synonym:

IQ-1

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 265 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 247.25
Formula C15H9N3O
CAS Number 23146-22-7
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

A novel dual NO-donating oxime and c-Jun N-terminal kinase inhibitor protects against cerebral ischemia-reperfusion injury in mice.
Atochin DN, et al. Neurosci Lett. 2016 Apr 8;618:45-49. PMID: 26923672.

Anti-Inflammatory Effects and Joint Protection in Collagen-Induced Arthritis after Treatment with IQ-1S, a Selective c-Jun N-Terminal Kinase Inhibitor.
Schepetkin IA, et al. J Pharmacol Exp Ther. 2015 Jun;353(3):505-16. PMID: 25784649.

Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
Schepetkin IA, et al. Mol Pharmacol. 2012 Jun;81(6):832-45. PMID: 22434859.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: IQ-1S, IQ-1 supplier, JNK, inhibitors

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