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IQ-1S free acid

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Chemical Structure| 23146-22-7 同义名 : IQ-1S (free acid);IQ-1S;IQ-1
CAS号 : 23146-22-7
货号 : A117837
分子式 : C15H9N3O
纯度 : 98%
分子量 : 247.251
MDL号 : MFCD00612483
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(64.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JNK1

    JNK1, IC50:390 nM

  • JNK2

    JNK2, IC50:360 nM

  • JNK3

    JNK3, IC50:87 nM
描述 The activating protein 1 (AP-1) and nuclear factor-κB (NF-κB) families of transcription factors are implicated in many pathological processes. C-Jun N-terminal kinases (JNKs) have been shown to regulate the transcriptional activity of AP-1. IQ-1S free acid is a potent inhibitor of pro-inflammatory cytokines without cytotoxic effect. It inhibits NF-κB/AP-1 activity with an IC50 value of 2.3±0.41μM. Treatment of human peripheral blood mononuclear cells with IQ-1S free acid (20μM) significantly inhibited LPS (200ng/ml)-induced production of pro-inflammatory cytokines, including IL-1α, IL-1β, IL-6, IL-10, and TNF-α, compared to DMSO-treated controls. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human MonoMac-6 cells are 1.3±0.31 and 3.8±0.78μM, respectively. The IC50 values of IQ-1S free acid for TNF-α and IL-6 in human peripheral blood mononuclear cells are 2.6±0.63 and 5.6±1.1μM, respectively. The IC50 values of IQ-1S free acid for NO in murine J774.A1 cells is 3.1±0.87μM. The binding affinity of IQ-1S free acid for JNK1, JNK2, and JNK3 are 0.24, 0.36, and 0.10μM, respectively. IQ-1S free acid also exhibits binding affinity towards CK1δ, PI3Kγ, and MKNK2 with Kd values of 0.38, 0.47, and 0.92μM, respectively. When mice were i.p. administered with IQ-1S free acid at a dose of 12.5 and 30mg/kg, the serum AUC0-12h values were 2.9 and 7.4μM/h, respectively. The i.p. injection of OVA-challenged mice with 12.5mg/kg IQ-1S free acid (every 12 h, a total of 5 injections) significantly suppressed OVA-induced CD4+ T-cell immune response compared to the vehicle-treated group[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.04mL

0.81mL

0.40mL

20.22mL

4.04mL

2.02mL

40.44mL

8.09mL

4.04mL
参考文献

[1]Atochin DN, Schepetkin IA, et al. A novel dual NO-donating oxime and c-Jun N-terminal kinase inhibitor protects against cerebral ischemia-reperfusion injury in mice. Neurosci Lett. 2016 Apr 8;618:45-49.

[2]Schepetkin IA, Kirpotina LN, et al. Anti-Inflammatory Effects and Joint Protection in Collagen-Induced Arthritis after Treatment with IQ-1S, a Selective c-Jun N-Terminal Kinase Inhibitor. J Pharmacol Exp Ther. 2015 Jun;353(3):505-16.

[3]Schepetkin IA, Kirpotina LN, Khlebnikov AI, et al. Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol. 2012;81(6):832-845. doi:10.1124/mol.111.077446