2. MAPK/ERK Pathway Metabolic Enzyme/Protease Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor
  3. MNK PPAR Eukaryotic Initiation Factor (eIF) Stearoyl-CoA Desaturase (SCD)
  4. HD202A

HD202A 是一种口服有效、选择性的 MNK1/MNK2 双重抑制剂 (IC50 分别为 6.09 nM 和 8.06 nM；Kd 分别为 1.913 μM 和 5.244 μM)，并抑制 MNK-eIF4E 信号通路。HD202A 通过下调围脂滴蛋白 2 和 SCD1，同时上调脂肪甘油三酯脂酶和 PPARγ 辅激活因子 1α，从而增强线粒体脂肪酸氧化及氧化还原稳态。HD202A 可有效抑制了体重增加、肝脏脂质蓄积及血清脂质升高，还显著增强了机体的葡萄糖耐量与胰岛素敏感性，并改善了炎症特征。HD202A 展现出在代谢功能障碍相关脂肪性肝病研究中的重要应用潜力。

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HD202A

HD202A Chemical Structure

CAS No. : 2930131-74-9

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HD202A 相关抗体

Top Publications Citing Use of Products

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MNK1 MNK2 MNK

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, and Kd values of 1.913 μM and 5.244 μM, respectively) that inhibits the MNK-eIF4E signaling pathway. By downregulating perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α, HD202A enhances mitochondrial fatty acid oxidation and redox homeostasis. HD202A effectively suppresses body weight gain, hepatic lipid accumulation and elevation of serum lipids, significantly improves glucose tolerance and insulin sensitivity of the organism, and ameliorates inflammatory features. With these comprehensive pharmacological activities, HD202A exhibits great application potential in studies of metabolic dysfunction-associated steatotic liver disease[1].

IC50 & Target

MNK1

6.09 nM (IC50)

MNK2

8.06 nM (IC50)

PPARγ1

 

eIF4E

 

MNK1

1.913 μM (Kd)

MNK2

5.244 μM (Kd)

体外研究
(In Vitro)

HD202A (compound 26) (0.1-1 μM) 以剂量依赖的方式抑制 A549 细胞中 MNK 介导的 eIF4E 磷酸化[1]。
HD202A (1 μM) 可减少分化 3T3-L1 脂肪细胞中的脂滴积累并下调 Plin2，且无细胞毒性[1]。
HD202A (1 μM-25 μM; 24-36 h) 可减少 Palmitate (400 μM) 诱导的 HepG2 细胞中的脂质蓄积、恢复脂质稳态并改善线粒体功能；在 25 μM 浓度下，可抑制 HepG2 细胞增殖[1]。

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

HD202A 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HepG2 cells
Concentration: 25 μM; with or without 400 μM Palmitate
Incubation Time: 24-36 h
Result: Inhibited HepG2 cell proliferation by ~40%.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t AUC0-∞ T1/2 Bioavailability
Mice[1] 50 mg/kg i.g. 7.00 h 2256 ng/mL 27996 ng·h/mL 28367 ng·h/mL 3.13 h 42.1 %
Mice[1] 25 mg/kg i.v. 0.22 h 41583 ng/mL 133124 ng·h/mL 138348 ng·h/mL 5.39 h /
体内研究
(In Vivo)

HD202A (compound 26) (12.5-50 mg/kg；口服；每日；11 周) 可通过抑制 MNK-eIF4E 信号通路、改善脂质代谢、增强线粒体功能及减轻炎症反应，呈剂量依赖性缓解雄性 C57BL/6J 小鼠中高脂饮食 (HFD) 诱导的代谢相关脂肪性肝病 (MASLD)[1]。
HD202A (25-75 mg/kg；口服；单次) 在给药 24 小时后检测时，对小鼠白色脂肪组织、肝脏和骨骼肌具有体内 MNK 抑制活性[1]。

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

Animal Model: C57BL/6J (male, 20 weeks old, mean body weight ~48 g, HFD-induced MASLD)[1]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 11 weeks
Result: Attenuated HFD-induced body weight gain dose-dependently without altering food intake.
Reduced fat mass and increased lean mass.
Decreased liver, epididymal fat, and (at 50 mg/kg only) subcutaneous fat indices.
Improved glucose homeostasis dose-dependently, with faster glucose clearance and reduced AUC in ITT and OGTT at 50 mg/kg.
Reduced fasting glucose, serum TG, TC, LDL-C, NEFA, ALT, AST, and TNF-α levels across relevant doses.
Reduced hepatic triglyceride content and macrovesicular steatosis dose-dependently.
Decreased hepatic iNOS H-scores and increased hepatic CD163 H-scores (without changing F4/80 levels) at 50 mg/kg.
Suppressed hepatic P-eIF4E levels.
Downregulated SCD1 and Plin2 expression.
Upregulated ATGL and PGC-1α expression.
分子量

456.56

Formula

C25H24N6OS
CAS 号
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

HD202A 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

HD202A2930131-74-9MNKPPAREukaryotic Initiation Factor (eIF)Stearoyl-CoA Desaturase (SCD)Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePeroxisome proliferator-activated receptorsadipose triglyceride lipase3T3-L1 adipocytesA549 cellsHepG2 cellsperilipin 2MNK2peroxisome proliferator-activated receptor gamma coactivator 1αeIF4EMNK1stearoyl-coenzyme A desaturase 1Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-182046
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