2. MAPK/ERK Pathway
  3. JNK
  4. IQ-1S free acid

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.

IQ-1S free acid Chemical Structure

IQ-1S free acid Chemical Structure

CAS No. : 23146-22-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of IQ-1S free acid:

IQ-1S free acid Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE IQ-1S free acid

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  • Protocol

  • Purity & Documentation

  • References

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Description

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.

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)

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.

IQ-1S free acid Related Antibodies
In Vivo

When mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1S) i.p., the serum exposure of the compound is also good, with AUC0-12h values of 2.9 and 7.4 μM/h, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

247.25

Formula

C15H9N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.28%

SDS (393 KB)

COA (255 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
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IQ-1S free acid Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IQ-1S23146-22-7JNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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