A cell-permeable indenoquinoxalinone-oxime (IQ) compound that acts as a potent, non-toxic, reversible, ATP-competitive, high-affinity inhibitor of JNK (=390, 360 and 87nM for JNK1, JNK2 and JNK3, respectively) with moderate selectivity over CK1d, PI 3-Ky, and MKNK2 (IC50=1.4, 1.2, and 1.8uM, respectively). Shown to reduce c-Jun-Ser63 phosphorylation, and block the production of LPS-induced TNF-a (IC50 = 250nM) and IL-6 (IC50=610nM) in MonoMac-6 monocytic cells and in human hPBMCs, respectively. Also shown to inhibit NF-kB/AP-1 reporter activity (IC50=1.8uM) in human THP1-Blue monocytic cells and diminish nitric oxide production in murine J774-A.1 macrophages (IC50=12.5uM). Exhibits favorable pharmacokinetics properties and efficiently reduces ovalbumin-induced CD+ T-cell immune inflammation in a murine delayed-type hypersensitivity model (12.5mg/kg, two per day dosage, i.p.) Molecular Formula: C15H8N3Ona Primary Target: JNK1,2,3 Secondary Target: PI 3-Kg, CK1d and MKNK2 Solubility: DMSO Molecular Weight: 269.2 Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
269.2
Purity:
95% (HPLC)
Form:
Supplied as a bright yellow solid.
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