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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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IQ-1S is a potent and selective c-Jun N-Terminal Kinase Inhibitor. IQ-1S inhibits delayed-type hypersensitivity in mice. The most prevalent species at physiologic pH is IQ-1S, which has a high level of specificity for JNK. With regard to rheumatoid arthritis, IQ-1S can be used as a small-molecule modulator for mechanistic studies of JNK function by reducing the inflammation and cartilage loss that are caused by CIA.
| Targets |
JNK3 (IC50 = 87 nM nM); JNK2 (IC50 = 360 nM); JNK1 (IC50 = 390 nM)
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|---|---|
| ln Vitro |
Compound IQ-1S is a potent, noncytotoxic inhibitor of pro-inflammatory cytokine [interleukin (IL)-1α, IL-1β, IL-6, IL-10, tumor necrosis factor (TNF)-α, interferon-γ, and granulocyte-macrophage colony-stimulating factor] and nitric oxide production by human and murine monocyte/macrophages. Evaluation of IQ-1S' impact on human PBMCs' LPS-induced cytokine production. LPS (200 ng/mL) consistently induces five of the 12 cytokines examined (IL-1α, IL-1β, IL-6, IL-10, and TNF-α) in PBMCs when compared to DMSO-treated control cells. 20 M IQ-1S significantly reduces the production of each of these cytokines. TNF-α production is completely prevented by IQ-1 (>99%), IL-1α, IL-1β, and IL-10 levels are all reduced by 85%, and IL-6 production is reduced by 33%[1].
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| ln Vivo |
The serum exposure of the drug is also good when given to mice via intraperitoneal injection at doses of 12.5 and 30 mg/kg of IQ-1S (the sodium salt of IQ-1S), with AUC0-12h values of 2.9 and 7.4 μM/h, respectively[1].
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| Cell Assay |
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. Pretreatment of PBMCs with 20 μM IQ-1S or DMSO for 30 min is followed by the addition of 200 ng/ml LPS for 24 h. A human cytokine MultiAnalyte ELISArray Kit is used to analyze different 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 PBMC supernatants[1].
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| Animal Protocol |
Mice: For in vivo analysis, BALB/c mice (15–20 animals per group) are given 12.5 or 30 mg/kg i.p. doses of IQ-1S (the sodium salt of IQ-1), and the mice are sacrificed at different intervals after compound administration. For quantification, mouse serum samples spiked with known concentrations of IQ-1S (0.1–20 μM) are used to create a calibration curve, and a linear dependence of the peak area with IQ-1S concentration is discovered (correlation coefficient r=0.997). The linear trapezoidal method is used to calculate the area under the serum concentration-time curve (AUC0-12h) up to the last concentration that was measured[1].
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| References |
| Molecular Formula |
C15H9N3O
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|---|---|
| Molecular Weight |
247.2515
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| Exact Mass |
247.07
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| Elemental Analysis |
C, 72.87; H, 3.67; N, 16.99; O, 6.47
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| CAS # |
23146-22-7
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| Related CAS # |
23146-22-7
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C2C(=C1)C(=C3C2=NC4=CC=CC=C4N3)N=O
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| InChi Key |
YSYIWCNPSZNNKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9N3O/c19-18-14-10-6-2-1-5-9(10)13-15(14)17-12-8-4-3-7-11(12)16-13/h1-8,17H
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| Chemical Name |
11-nitroso-10H-indeno[1,2-b]quinoxaline
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| Synonyms |
IQ-1S
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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: ~16.7 mg/mL (~67.4 mM)
Ethanol: ~1 mg/mL (~4.0 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 16.7 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: 1.67 mg/mL (6.75 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL | |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.0890 mL | |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 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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