2. MAPK/ERK Pathway Cell Cycle/DNA Damage NF-κB
  3. MNK Eukaryotic Initiation Factor (eIF) NF-κB
  4. MNK1/2-IN-10

MNK1/2-IN-10 是一种口服有效的、选择性的 MNK1/MNK2 抑制剂，对 MNK1 的 IC50 为 10.84 nM，对 MNK2 的 IC50 为 12.81 nM。MNK1/2-IN-10 可抑制 eIF4E 磷酸化、NF-κB 信号通路、巨噬细胞极化、氧化应激及促炎细胞因子的产生。MNK1/2-IN-10 可减轻 LPS (HY-D1056) 诱导的炎症小鼠模型中的肾脏和脾脏损伤。MNK1/2-IN-10 可用于急性炎症相关研究。

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MNK1/2-IN-10

MNK1/2-IN-10 Chemical Structure

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MNK1/2-IN-10 相关抗体

Top Publications Citing Use of Products

查看 MNK 亚型特异性产品:

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MNK1 MNK2 MNK

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MNK1/2-IN-10 is an orally active, selective MNK1/MNK2 inhibitor, with an IC50 of 10.84 nM for MNK1 and an IC50 of 12.81 nM for MNK2. MNK1/2-IN-10 inhibits eIF4E phosphorylation, the NF-κB signaling pathway, macrophage polarization, oxidative stress and the production of pro-inflammatory cytokines. MNK1/2-IN-10 alleviates kidney and spleen damage in LPS (HY-D1056)-induced inflammatory mouse models. Anti-inflammatory agent 115 is applicable for research related to acute inflammation[1].

IC50 & Target[1]

MNK1

10.84 nM (IC50)

MNK2

12.81 nM (IC50)

体外研究
(In Vitro)

MNK1/2-IN-10 (Compound 13) (48 h) 在 RAW 264.7、HEK293T、HUVECs 和 AML-12 细胞系中细胞毒性较低，孵育 48 h 后的 IC50 值介于 24.25 至 77.56 μM 之间[1]。
MNK1/2-IN-10 (1.25-10 μM; 24 h) 以浓度依赖的方式抑制 RAW 264.7 细胞中 LPS 诱导的 p-eIF4E 和 iNOS 表达[1]。
MNK1/2-IN-10 (1.25-10 μM; 4 h) 可浓度依赖性地抑制 LPS 诱导的 RAW 264.7 细胞中 p-eIF4E 的表达[1]。
MNK1/2-IN-10 (1.25-10 μM; 24 h) 可呈浓度依赖性抑制 RAW 264.7 细胞中 LPS 诱导的 IL-6、TNF-α 和 MCP-1 的释放[1]。
MNK1/2-IN-10 (1.25-10 μM; 24 h) 可浓度依赖性地抑制 LPS 诱导的 RAW 264.7 细胞中一氧化氮释放，在 10 μM 时抑制作用达到最大[1]。
MNK1/2-IN-10 (10 μM; 24 h) 可抑制 RAW 264.7 细胞中 LPS 诱导的 iNOS 表达[1]。
MNK1/2-IN-10 (1.25-10 μM; 12 h) 可在体外以浓度依赖的方式抑制 LPS 诱导的 RAW 264.7 细胞中 NF-κB 通路的激活[1]。
MNK1/2-IN-10 (10 μM; 24 h) 可抑制 LPS 诱导的 RAW 264.7 细胞中 P65 的核转位[1]。
MNK1/2-IN-10 (2.5-10 μM; 13 h) 可呈浓度依赖性降低 RAW 264.7 细胞中 LPS 诱导的 ROS 生成[1]。
MNK1/2-IN-10 (10 μM; 14 h) 可抑制 RAW 264.7 细胞中 LPS 诱导的 ROS 生成[1]。
MNK1/2-IN-10 (2.5-10 μM; 24 h) 可在体外以浓度依赖的方式恢复 LPS 刺激的 RAW 264.7 细胞中 GSH 水平并增强 SOD 活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MNK1/2-IN-10 相关抗体:

Western Blot Analysis[1]

Cell Line: RAW 264.7
Concentration: 10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time: 24 h
Result: Suppressed LPS-induced phosphorylation of eIF4E in a concentration-dependent manner, with maximal suppression at 10 μM.
Suppressed LPS-induced expression of iNOS in a concentration-dependent manner, with maximal suppression at 10 μM.

Immunofluorescence[1]

Cell Line: RAW 264.7
Concentration: 10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time: 2 h (pretreatment); 2 h (LPS stimulation)
Result: Inhibited LPS-induced p-eIF4E expression in a concentration-dependent manner, as shown by reduced green fluorescence intensity.

ELISA Assay[1]

Cell Line: RAW 264.7
Concentration: 10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time: 24 h
Result: Inhibited LPS-induced secretion of IL-6 in a dose-dependent manner.
Inhibited LPS-induced secretion of TNF-α in a dose-dependent manner.
Inhibited LPS-induced secretion of MCP-1 in a dose-dependent manner.

Immunofluorescence[1]

Cell Line: RAW 264.7
Concentration: 10 μM
Incubation Time: 24 h
Result: Diminished iNOS signal in the cytoplasm of LPS-stimulated cells.

Western Blot Analysis[1]

Cell Line: RAW 264.7
Concentration: 10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time: 12 h
Result: Inhibited LPS-induced phosphorylation of P65 in a concentration-dependent manner.
Inhibited LPS-induced phosphorylation of IκBα in a concentration-dependent manner.

Immunofluorescence[1]

Cell Line: RAW 264.7
Concentration: 10 μM
Incubation Time: 12 h (pretreatment); 12 h (LPS stimulation)
Result: Blocked LPS-triggered nuclear translocation of P65, with significantly reduced fluorescence intensity in the nucleus.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC0-t Bioavailability
Rat[1] 10 mg/kg i.v. 17403.000 ng/mL 1.389 h 10.090 h 82007.297 ng·h/mL /
Rat[1] 200 mg/kg p.o. 5833.000 ng/mL 2.167 h 15.951 h 107535.552 ng·h/mL 6.6 %
体内研究
(In Vivo)

MNK1/2-IN-10 (Compound 13) (25-100 mg/kg；口服；每日一次；16 天) 可强效缓解雄性 C57BL/6J 小鼠中 LPS 诱导的急性炎症与器官损伤，其中 100 mg/kg 剂量在促炎细胞因子减少、p-eIF4E 与 iNOS 表达抑制、抗氧化功能恢复及组织病理学改善方面展现出最强效力[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 6−8 weeks old, 18−21 g, LPS-induced)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 16 days
Result: Significantly reduced LPS-induced kidney and spleen indices, with the 100 mg/kg dose showing the strongest effect.
Improved renal function, reducing serum creatinine and urea nitrogen levels; the 50 and 100 mg/kg doses showed greater improvement than the positive control dexamethasone.
Mitigated LPS-induced kidney pathological changes (tubular dilation, brush border necrosis, vacuolization, structural disruption) and spleen pathological changes (nuclear swelling, cellular edema, inflammatory infiltration, microcirculatory dysfunction).
Significantly reduced serum levels of pro-inflammatory cytokines TNF-α, IL-6, MCP-1, and IL-1β, with the 100 mg/kg dose showing the strongest suppression.
Significantly suppressed p-eIF4E expression and downregulated the M1 macrophage marker iNOS in kidney and spleen tissues, with the 100 mg/kg dose showing the strongest effect.
Restored antioxidant capacity by increasing glutathione and superoxide dismutase levels, and reduced lipid peroxidation by lowering malondialdehyde levels in tissues.
分子量

520.63

Formula

C25H24N6O3S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MNK1/2-IN-10 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MNK1/2-IN-10MNKEukaryotic Initiation Factor (eIF)NF-κBMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseNuclear factor-κBNuclear factor-kappaBHUVECsoxidative stressC57BL/6J miceMNK1RAW 264.7NF-κB signalingeIF4E phosphorylationMNK2macrophage polarizationHEK293TInhibitorinhibitorinhibit

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