| Bioactivity | IQ-1S is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 1.8 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 87 nM, 360 nM, and 390 nM for JNK3, JNK2, and JNK1, respectively. |
| Invitro | IQ-1S（IQ-1 的钠盐）是一种强效、无细胞毒性的促炎细胞因子 [IL-1α、IL-1β、IL-6、IL-10、TNF-α、干扰素-γ 和 GM-CSF)] 和人类和鼠单核细胞/巨噬细胞产生的一氧化氮抑制剂。评估了 IQ-1 对 LPS 诱导的人类 PBMC 细胞因子产生的影响。在所分析的 12 种细胞因子中，与 DMSO 处理的对照细胞相比，LPS (200 ng/mL) 在 PBMC 中持续诱导五种细胞因子 (IL-1α、IL-1β、IL-6、IL-10 和 TNF-α)。20 μM IQ-1 可显著抑制所有这些细胞因子的产生。其中，TNF-α 的产生被 IQ-1 完全抑制 (>99%)，IL-1α、IL-1β 和 IL-10 的水平降低 85%，IL-6 的产生降低 33%。 IQ-1S 抑制 MonoMac-6 细胞中 LPS 诱导的 TNF-α 和 IL-6 的产生，IC50 值分别为 0.25 和 0.61 μM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> IQ-1S 相关抗体: |
| In Vivo | 小鼠腹腔注射 12.5 和 30 mg/kg IQ-1S（IQ-1 的钠盐）时，该化合物的血清暴露量也很好，AUC0-12h 值分别为 2.9 和 7.4 μM/h[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 1421610-21-0 |
| Formula | C15H8N3NaO |
| Molar Mass | 269.23 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Schepetkin IA, et al. Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol. 2012 Jun;81(6):832-45. |