IQ-1S free acid
Based on 1 publication(s) in Google Scholar
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
For research use only. We do not sell to patients.
- Purity : 99.28%
- CAS No.: 23146-22-7
- Formula: C15H9N3O
- Molecular Weight:247.25
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) IQ-1S free acid
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Biological Activity
Description
IC50 & Target
[1]|
JNK3 100 nM (Kd) |
JNK1 240 nM (Kd) |
JNK2 360 nM (Kd) |
CK1δ 0.38 μM (Kd) |
PI3Kγ 0.47 μM (Kd) |
MKNK2 0.92 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | IC50 |
>10 μM
Compound: 5a
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Antiproliferative activity against human HuH7 cells after 72 hrs by XTT assay
Antiproliferative activity against human HuH7 cells after 72 hrs by XTT assay
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[PMID: 26686931] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: 5a
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay
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[PMID: 26686931] |
| MONO-MAC-6 | IC50 |
3.8 μM
Compound: IQ-1
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Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
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[PMID: 30347329] |
| MRC5 | IC50 |
51.12 μM
Compound: 5a
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Antiproliferative activity against human MRC5 cells after 72 hrs by XTT assay
Antiproliferative activity against human MRC5 cells after 72 hrs by XTT assay
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[PMID: 26686931] |
| NCI-H1299 | IC50 |
>10 μM
Compound: 5a
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Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay
Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay
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[PMID: 26686931] |
| PC-3 | IC50 |
>10 μM
Compound: 5a
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Antiproliferative activity against human PC3 cells after 72 hrs by XTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by XTT assay
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[PMID: 26686931] |
In 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. 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%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 23146-22-7
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Appearance Solid
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Molecular Weight 247.25
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Formula C15H9N3O
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Color White to off-white
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SMILES
O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 16.67 mg/mL (67.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL | 101.1122 mL |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.0890 mL | 20.2224 mL | |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL | 10.1112 mL | |
| 15 mM | 0.2696 mL | 1.3482 mL | 2.6963 mL | 6.7408 mL | |
| 20 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL | 5.0556 mL | |
| 25 mM | 0.1618 mL | 0.8089 mL | 1.6178 mL | 4.0445 mL | |
| 30 mM | 0.1348 mL | 0.6741 mL | 1.3482 mL | 3.3704 mL | |
| 40 mM | 0.1011 mL | 0.5056 mL | 1.0111 mL | 2.5278 mL | |
| 50 mM | 0.0809 mL | 0.4044 mL | 0.8089 mL | 2.0222 mL | |
| 60 mM | 0.0674 mL | 0.3370 mL | 0.6741 mL | 1.6852 mL |
IQ-1S free acid Related Classifications
HY-100233 Related Classifications
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