IQ-1S
Based on 1 publication(s) in Google Scholar
IQ-1S is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 1.8 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 87 nM, 360 nM, and 390 nM for JNK3, JNK2, and JNK1, respectively.
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- No. CAS: 1421610-21-0
- Fòrmula: C15H8N3NaO
- Peso molecular:269.23
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Actividad biológica
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JNK3 87 nM (Kd) |
JNK2 360 nM (Kd) |
JNK1 390 nM (Kd) |
PI3Kγ 1.2 μM (Kd) |
CK1δ 1.4 μM (Kd) |
MKNK2 1.8 μM (Kd) |
IQ-1S (The sodium salt of IQ-1) is a potent, noncytotoxic inhibitor of pro-inflammatory cytokine [IL-1α, IL-1β, IL-6, IL-10, TNF-α, interferon-γ, and GM-CSF)] and nitric oxide production by human and murine monocyte/macrophages. The effect of IQ-1 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-1. 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%. IQ-1S inhibits LPS-induced TNF-α and IL-6 production in MonoMac-6 cells with IC50 values of 0.25 and 0.61 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1421610-21-0
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Peso molecular 269.23
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Fòrmula C15H8N3NaO
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SMILES
[Na]O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Protocolo
Kinase profiling is performed using a panel of 91 protein kinases. In brief, kinases are produced and displayed on T7 phage or expressed in HEK-293 cells. Binding reactions are performed at room temperature for 1 h, and the fraction of kinase not bind to test compound is determined by capture with an immobilized affinity ligand and quantified by quantitative polymerase chain reaction. Primary screening at fixed concentrations of compounds is performed in duplicate. Selected hit compounds are submitted for dissociation constant (Kd) determination using the same platform. For dissociation constant Kd determination, a 12-point half-log dilution series (a maximum concentration of 100 μM) is used. Assays are performed in duplicate, and their mean value is displayed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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-1S (The sodium salt of 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
For in vivo analysis, 12.5 or 30 mg/kg i.p. doses of IQ-1S (The sodium salt of IQ-1) are administered to BALB/c mice (15-20 animals/group), and the mice are sacrificed at various time points after compound administration. For quantification, a calibration curve is established using mouse serum samples spiked with known concentrations of IQ-1S (0.1-20 μM), and a linear dependence of the peak area with IQ-1S concentration is obtained (correlation coefficient r=0.997). The area under the serum concentration-time curve (AUC0-12h) is calculated using the linear trapezoidal method up to the last measured concentration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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