Pim1/AKK1-IN-1
(Synonyms: N-[5-(4-氰基苯基)-1H-吡咯并[2,3-B]吡啶-3-基]-3-吡啶甲酰胺,LKB1/AAK1 dual inhibitor) 目录号 : GC13154
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Pim1/AKK1-IN-1是一种有效的多靶点抑制剂，对Pim1、AKK1（AAK1）、LKB1和MST2等激酶具有抑制作用。
Cas No.:1093222-27-5
Sample solution is provided at 25 µL, 10mM.
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Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor that exerts inhibitory effects on kinases including Pim1, AKK1 (AAK1), LKB1 and MST2[1]. These kinases play key roles in regulating cell proliferation-apoptosis balance, endocytic transport, and energy metabolism[2][3]. Pim1/AKK1-IN-1 is usually used in metabolic and viral infection-related research[4][5].
In vitro, Pim1/AKK1-IN-1 (10-1000nM; 48h) dose-dependently reversed NaB-induced suppression of STAT6 phosphorylation, nuclear translocation, and IL-4R recruitment in bone marrow-derived macrophages[6].
In vivo, Pim1/AKK1-IN-1 (40mg/kg; single intraperitoneal injection) exacerbated DSS-induced colitis in mice, increased colonic UGT1A4 levels and bile acid accumulation, caused greater weight loss compared to DSS treatment alone[7].
References:
[1] Bamborough P, Drewry D, Harper G, Smith GK, Schneider K. Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem. 2008;51(24):7898-7914.
[2] Trelford CB, Shepherd TG. LKB1 biology: assessing the therapeutic relevancy of LKB1 inhibitors. Cell Commun Signal. 2024;22(1):310.
[3] Xin X, Wang Y, Zhang L, et al. Development and therapeutic potential of adaptor-associated kinase 1 inhibitors in human multifaceted diseases. Eur J Med Chem. 2023;248:115102.
[4] Zhou B, Luo Y, Ji N, Hu C, Lu Y. Orosomucoid 2 maintains hepatic lipid homeostasis through suppression of de novo lipogenesis. Nat Metab. 2022;4(9):1185-1201.
[5] Garcia-Carceles J, Caballero E, Gil C, Martinez A. Kinase Inhibitors as Underexplored Antiviral Agents. J Med Chem. 2022;65(2):935-954.
[6] Liang W, Wu H, Long Q, et al. LKB1 activated by NaB inhibits the IL-4/STAT6 axis and ameliorates renal fibrosis through the suppression of M2 macrophage polarization. Life Sci. 2025;370:123564.
[7] Lin Z, Feng Y, Wang J, Men Z, Ma X. Microbiota governs host chenodeoxycholic acid glucuronidation to ameliorate bile acid disorder induced diarrhea. Microbiome. 2025;13(1):36.
Pim1/AKK1-IN-1是一种有效的多靶点抑制剂，对Pim1、AKK1（AAK1）、LKB1和MST2等激酶具有抑制作用[1]。这些激酶在调节细胞增殖-凋亡平衡、内吞运输和能量代谢中起关键作用[2][3]。Pim1/AKK1-IN-1通常用于代谢和病毒感染相关研究[4][5]。
体外实验中，Pim1/AKK1-IN-1（10-1000nM; 48h）呈剂量依赖性逆转了NaB诱导的骨髓源性巨噬细胞中STAT6磷酸化、核易位和IL-4R募集的抑制[6]。
体内实验中，与单独DSS处理相比，Pim1/AKK1-IN-1 （40mg/kg；单次腹腔注射）加重DSS诱导的小鼠结肠炎，增加结肠UGT1A4水平和胆汁酸积累，引起更大的体重减轻[7]。
| Cell experiment [1]: | |
Cell lines | bone marrow-derived macrophages |
Preparation Method | Mononuclear cells were isolated from the femurs of 6-8 week-old C57BL/6J mice. The cells were plated in 10cm culture dishes and maintained in a medium containing 20ng/ml mouse macrophage colony-stimulating factor (M-CSF) for 5-7 days to generate bone marrow-derived macrophages (BMDM). Subsequently, BMDMs were stimulated 20ng/ml mouse IL-4 for 2h followed by treatment with NaB and/or Pim1/AKK1-IN-1 (10-1000nM) for 48h. STAT6 phosphorylation were analyzed by Western blot using anti-STAT6 antibody. |
Reaction Conditions | 10-1000nM; 48h |
Applications | Pim1/AKK1-IN-1 dose-dependently reversed NaB-induced suppression of STAT6 phosphorylation in bone marrow-derived macrophages. |
| Animal experiment [2]: | |
Animal models | male C57BL/6 mice |
Preparation Method | 5-week-old male C57BL/6 mice gained daily care with a 12h light/12h dark cycle. Mice were randomly divided into three groups (n=8 per group): Control (drinking water), DSS (saline by oral gavage), and DSS+LKB1 inhibitor (40mg/kg Pim1/AKK1-IN-1 by single intraperitoneal injection) . Subsequently these mice received 3% DSS daily drink for 7 days. Body weight was recorded, besides colonic tissue samples, colonic fixed samples, and colonic chyme samples were collected during sampling, liver and spleen were weighed, and colonic length was measured. |
Dosage form | 40mg/kg; single intraperitoneal injection |
Applications | Pim1/AKK1-IN-1 exacerbated DSS-induced colitis in mice model, caused greater weight loss compared to DSS treatment alone. |
References: | |
| Cas No. | 1093222-27-5 | SDF | |
| 别名 | N-[5-(4-氰基苯基)-1H-吡咯并[2,3-B]吡啶-3-基]-3-吡啶甲酰胺,LKB1/AAK1 dual inhibitor | ||
| 化学名 | N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide | ||
| Canonical SMILES | C1=CC(=CN=C1)C(=O)NC2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)C#N | ||
| 分子式 | C20H13N5O | 分子量 | 339.36 |
| 溶解度 | ≥ 34.8 mg/mL in DMSO | 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 | 2.9467 mL | 14.7336 mL | 29.4672 mL |
| 5 mM | 589.3 μL | 2.9467 mL | 5.8934 mL |
| 10 mM | 294.7 μL | 1.4734 mL | 2.9467 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
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet