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HD202A
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Catalog No. T218370 Copy Product Info
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HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, respectively; Kd values of 1.913 μM and 5.244 μM, respectively), and it 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. This compound effectively curtails weight gain, hepatic lipid accumulation, and elevated serum lipid levels, while significantly improving glucose tolerance and insulin sensitivity, and reducing inflammatory characteristics. HD202A shows significant potential for research applications in metabolic dysfunction-associated fatty liver disease.
HD202A
Cas No. 2930131-74-9
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | HD202A is an orally active, selective dual inhibitor of MNK1/MNK2 (with IC50 values of 6.09 nM and 8.06 nM, respectively; Kd values of 1.913 μM and 5.244 μM, respectively), and it 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. This compound effectively curtails weight gain, hepatic lipid accumulation, and elevated serum lipid levels, while significantly improving glucose tolerance and insulin sensitivity, and reducing inflammatory characteristics. HD202A shows significant potential for research applications in metabolic dysfunction-associated fatty liver disease. |
| Targets & IC50 | MNK1:6.09 nM |
| In vitro | HD202A (compound 26) inhibits eIF4E phosphorylation mediated by MNK in A549 cells in a dose-dependent manner at concentrations of 0.1-1 μM. At 1 μM, HD202A reduces lipid droplet accumulation in differentiated 3T3-L1 adipocytes and downregulates Plin2 without cytotoxic effects. Additionally, HD202A at 1 μM-25 μM, administered for 24-36 hours, decreases palmitate (400 μM)-induced lipid accumulation in HepG2 cells, restores lipid homeostasis, and improves mitochondrial function, with a 25 μM concentration inhibiting HepG2 cell proliferation. |
| In vivo | HD202A (compound 26) administered orally at doses of 12.5-50 mg/kg daily for 11 weeks demonstrates dose-dependent alleviation of high-fat diet (HFD)-induced metabolic-associated steatotic liver disease (MASLD) in male C57BL/6J mice. This effect occurs through the inhibition of the MNK-eIF4E signaling pathway, improvement of lipid metabolism, enhancement of mitochondrial function, and reduction of inflammation. Additionally, a single oral dose of HD202A (25-75 mg/kg) shows in vivo MNK inhibitory activity in mouse white adipose tissue, liver, and skeletal muscle 24 hours post-administration. |
| Molecular Weight | 456.56 |
| Formula | C25H24N6OS |
| Cas No. | 2930131-74-9 |
| Smiles | N#CC=1C=CC(=CC1)C2=CN=C3SC(=NN32)C=4C=CC(=CC4)C(=O)N5CCC(N(C)C)CC5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: HD202A in vivo | HD202A in vitro | HD202A formula | HD202A molecular weight
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