IQ-1S

Research use only, not for human use.

A potent, highly specific JNK inhibitor with IC50 of 390, 360, and 87 nM for JNK1, JNK2, and JNK3, respectively.

A potent, highly specific JNK inhibitor with IC50 of 390, 360, and 87 nM for JNK1, JNK2, and JNK3, respectively; does not inhibits other kinases that represent potential targets for RA treatment, including GSK-3beta, JAK2, JAK3, PI3Ks, Btk, IKK-2, etc.; inhibits pro-inflammatory cytokine (IL-1α, IL-1β, IL-6, IL-10, TNF-α, IFN-γ, and GM-CSF and nitric oxide production by human and murine monocyte/macrophages; inhibits LPS-induced TNF-α and IL-6 production in MonoMac-6 cells with IC50 of 0.25 and 0.61 uM, respectively; reduces inflammation and cartilage loss associated with CIA in mice model.

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%.

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.

IQ 1S free acid

MAPK/ERK Signaling

JNK

JNK1|JNK2|JNK3

Neurological Disease

——

23146-22-7

247.2515

C15H9N3O

>98% (HPLC)

DMSO: ≥ 32 mg/mL

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

11H-Indeno[1,2-b]quinoxalin-11-one, oxime

(-20℃)

With Ice Pack

≥ 2 years