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CAS No.: 23146-22-7

IQ-1S free acid Catalog No. CSN18143

Synonyms: IQ-1S (free acid);IQ-1;IQ-1S

IQ-1S Free Acid is a selective JNK3 inhibitor with IC50 value of 87 nM, with less potency against JNK 1/2 with IC50 values of 390/360nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JNK2

Kd:360nM JNK1

Kd:390nM JNK3

Kd:87nM
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 K_d 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 AUC_0-12h 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0445 mL
- 20.2223 mL
- 40.4446 mL
- 5 mM
- 0.8089 mL
- 4.0445 mL
- 8.0889 mL
- 10 mM
- 0.4044 mL
- 2.0222 mL
- 4.0445 mL

技术信息

CAS号

23146-22-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H9N3O

运输

蓝冰

分子量

247.25

别名

IQ-1S (free acid);IQ-1;IQ-1S

溶解度

DMSO	46.0 mg/mL (186.0 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (4.0 mM)

动物实验配方

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靶点	Description	IC50
JNK2		Kd:360nM
JNK1		Kd:390nM
JNK3		Kd:87nM

IQ-1S free acid Catalog No. CSN18143

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