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IQ-1S

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Catalog No. T203575Cas No. 1421610-21-0

IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.

IQ-1S

IQ-1S

😃Good
Catalog No. T203575Cas No. 1421610-21-0
IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.
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50 mgInquiry10-14 weeks
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Product Introduction

Bioactivity
Description
IQ-1S is an inhibitor of NF-κB/activating protein 1 (AP-1) with an IC50 of 1.8 μM. It exhibits high binding affinity to all three JNKs, with Kd values for JNK3, JNK2, and JNK1 being 87 nM, 360 nM, and 390 nM, respectively.
Targets&IC50
CK1δ:1.4 μM (Kd), JNK1:390 nM (Kd), JNK2:360 nM (Kd), PI3Kγ:1.2 μM (Kd), MKNK2:1.8 μM (Kd), JNK3:87 nM (Kd)
In vitro
IQ-1S (the sodium salt of IQ-1) is a potent, non-cytotoxic inhibitor of pro-inflammatory cytokines [IL-1α, IL-1β, IL-6, IL-10, TNF-α, interferon-γ, and GM-CSF], as well as nitric oxide produced by human and mouse monocytes/macrophages. The impact of IQ-1 on LPS-induced cytokine production in human PBMCs was evaluated. Among the 12 cytokines analyzed, LPS (200 ng/mL) consistently induced the production of five cytokines (IL-1α, IL-1β, IL-6, IL-10, and TNF-α) in PBMCs compared to DMSO-treated control cells. At a concentration of 20 μM, IQ-1 significantly inhibited the production of all these cytokines. Notably, TNF-α production was nearly completely suppressed (>99%) by IQ-1, while levels of IL-1α, IL-1β, and IL-10 were reduced by 85%, and IL-6 production decreased by 33%.
In vivo
When administered via intraperitoneal injection in mice at doses of 12.5 and 30 mg/kg, IQ-1S (sodium salt of IQ-1) demonstrated adequate serum exposure, with AUC 0-12h values of 2.9 and 7.4 μM/h, respectively.
Chemical Properties
Molecular Weight269.23
FormulaC15H8N3NaO
Cas No.1421610-21-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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