IQ-1S

SKU: orb1225579

Description

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.

Images & Validation

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Key Properties

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CAS Number	23146-22-7
MW	247.2515
Purity	>98% (HPLC)
Formula	C₁₅H₉N₃O
SMILES	O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2
Target	JNK
Solubility	DMSO: ≥ 32 mg/mL

Bioactivity

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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.

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%.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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IQ 1S free acid

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Gene Symbol

JNK

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IQ-1S (orb1225579)

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Purity:	>98%
CAS Number:	1421610-21-0
MW:	269.23
Formula:	C₁₅H₈N₃O ∙ Na

Purity:	97.82%
CAS Number:	23146-22-7
MW:	247.25
Formula:	C₁₅H₉N₃O

CAS Number:	1421610-21-0
MW:	269.23
Formula:	C₁₅H₈N₃NaO

IQ-1S

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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IQ-1S (orb1225579)

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