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

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.

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HD202A

HD202A Chemical Structure

CAS No. : 2930131-74-9

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HD202A Related Antibodies

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Description

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)

In Vitro

HD202A (compound 26) (0.1-1 μM) dose-dependently inhibits MNK-mediated eIF4E phosphorylation in A549 cells[1].
HD202A (1 μM) reduces lipid droplet accumulation and downregulates Plin2 in differentiated 3T3-L1 adipocytes without causing cytotoxicity[1].
HD202A (1 μM; 24-36 h) reduces lipid accumulation, restores lipid homeostasis, and improves mitochondrial function in PA-induced HepG2 cells; at 25 μM, it inhibits HepG2 cell proliferation[1].

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

HD202A Related Antibodies

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%.
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 /
In Vivo

HD202A (compound 26) (12.5-50 mg/kg; p.o.; daily; 11 weeks) dose-dependently attenuates HFD-induced MASLD in male C57BL/6J mice by suppressing MNK-eIF4E signaling, improving lipid metabolism, enhancing mitochondrial function, and reducing inflammation, with the most pronounced effects observed at the 50 mg/kg daily oral dose[1].
HD202A (25-75 mg/kg; p.o.; single dose) exhibits in vivo MNK inhibitory activity in white adipose tissue, liver, and skeletal muscle of mice when measured 24 hours postdose[1].

MedChemExpress (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.
Molecular Weight

456.56

Formula

C25H24N6OS
CAS No.
SMILES

O=C(N1CCC(N(C)C)CC1)C2=CC=C(C3=NN4C(S3)=NC=C4C5=CC=C(C#N)C=C5)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HD202A Related Classifications

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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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