420149
JNK Inhibitor XV, IQ-1S
The JNK Inhibitor XV, IQ-1S controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
11H-Indeno[1,2-b]quinoxalin-11-one oxime, sodium salt
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About This Item
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
bright yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Packaging
Packaged under inert gas
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JNK1,2,3
JNK1,2,3
Reversible: yes
Secondary Target
PI 3-Kγ, CK1δ and MKNK2
PI 3-Kγ, CK1δ and MKNK2
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable indenoquinoxalinone-oxime (IQ) compound that acts as a potent, non-toxic, reversible, ATP-competitive, high-affinity inhibitor of JNK (Kd = 390, 360 and 87 nM for JNK1, JNK2 and JNK3, respectively) with moderate selectivity over CK1δ, PI 3-Kγ, and MKNK2 (IC50 = 1.4, 1.2, and 1.8 µM, respectively). Shown to reduce c-Jun-Ser63 phosphorylation, and block the production of LPS-induced TNF-α (IC50 = 250 nM) and IL-6 (IC50 = 610 nM) in MonoMac-6 monocytic cells and in human hPBMCs, respectively. Also shown to inhibit NF-κB/AP-1 reporter activity (IC50 = 1.8 µM) in human THP1-Blue monocytic cells and diminish nitric oxide production in murine J774-A.1 macrophages (IC50 = 12.5 µM). Exhibits favorable pharmacokinetics properties and efficiently reduces ovalbumin-induced CD+ T-cell immune inflammation in a murine delayed-type hypersensitivity model (12.5 mg/kg, two per day dosage, i.p.).
Other Notes
Schepetkin, I.A., et al. 2012. Mol. Pharmacol.81, 832.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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