IQ-1S free acid
(Synonyms: 11H-茚并[1,2-b]喹喔啉-11-酮肟) 目录号 : GC36327
An inhibitor of NF-κB/AP-1
Cas No.:23146-22-7
Sample solution is provided at 25 µL, 10mM.
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IQ-1S (free acid) is an inhibitor of NF-κB/AP-1 (IC50 = 2.3 ?M in a reporter assay).1 It inhibits TNF-α and IL-6 production in human Mono-Mac-6 cells (IC50s = 1.3 and 3.8 ?M, respectively) and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2.6 and 5.6 ?M, respectively), as well as nitric oxide (NO) production in murine J774-A.1 macrophages (IC50 = 3.1 ?M). IQ-1S (free acid) binds to JNKs (Kd = 0.24, 0.36, and 0.1?M for JNK1-3), as well as casein kinase 1δ (CK1δ), PI3Kγ, and MAPK-interacting serine/threonine kinase 2 (MKNK2; Kds = 0.38, 0.47, and 0.92 ?M, respectively).
1.Schepetkin, I.A., Kirpotina, L.N., Khlebnikov, A.I., et al.Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitorsMol. Pharmacol.81(6)832-845(2012)
Cell experiment: | Human PBMCs are plated in 96-well plates at a density of 2×105 cells/well in culture medium supplemented with 3% (v/v) endotoxin-free FBS. PBMCs are pretreated with 20 μM IQ-1S or DMSO for 30 min, followed by addition of 200 ng/ml LPS for 24 h. A human cytokine MultiAnalyte ELISArray Kit is used to evaluate various cytokines (IL-1α, IL-1β, IL-2, IL-4, IL-6, IL-8, IL-10, IL-12, IL-17A, interferon (IFN)-γ, TNF-α, and granulocyte-macrophage colony-stimulating factor in supernatants of PBMCs[1]. |
Animal experiment: | Mice[1]For in vivo analysis, 12.5 or 30 mg/kg i.p. doses of IQ-1S (The sodium salt of IQ-1) are administered to BALB/c mice (15-20 animals/group), and the mice are sacrificed at various time points after compound administration. For quantification, a calibration curve is established using mouse serum samples spiked with known concentrations of IQ-1S (0.1-20 μM), and a linear dependence of the peak area with IQ-1S concentration is obtained (correlation coefficient r=0.997). The area under the serum concentration-time curve (AUC0-12h) is calculated using the linear trapezoidal method up to the last measured concentration[1]. |
References: [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. | |
| Cas No. | 23146-22-7 | SDF | |
| 别名 | 11H-茚并[1,2-b]喹喔啉-11-酮肟 | ||
| Canonical SMILES | O/N=C1C2=C(C3=NC4=CC=CC=C4N=C3\1)C=CC=C2 | ||
| 分子式 | C15H9N3O | 分子量 | 247.25 |
| 溶解度 | DMSO: ≥ 32 mg/mL (129.42 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.089 mL |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet