1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. ZG-2291

ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases.

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ZG-2291 Chemical Structure

ZG-2291 Chemical Structure

CAS No. : 2962103-40-6

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Description

ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases[1].

In Vitro

ZG-2291 (5 and 20 μM, 48 h) is an active cell-penetrating FIH inhibitor in Hep3B cells[1].
ZG-2291 (5 and 20 μM, 48 h) promotes thermogenesis and improves lipid accumulation in 3T3-L1-derived adipocytes[1].

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

Real Time qPCR[1]

Cell Line: Hep3B cells
Concentration: 5, 20 μM
Incubation Time: 48 h
Result: Clearly upregulated the expression of the HIF target gene EGLN3, while the upregulation effect on other HIF target genes such as SLC2A1, BNIP3, and EPO was relatively mild.
In Vivo

ZG-2291 (10 mg/kg, i.p., every other day for 30 days) protects against the effects of obesity and notably improves obesity-associated metabolic dysfunction in ob/ob mice[1].

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

Animal Model: ob/ob mice
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day for a total of 30 days
Result: Resulted in lower body weight, reduced hepatic TG/TC, and lower serum TG/TC/low-density lipoprotein (LDL) cholesterol levels in mice compared to the control group
Molecular Weight

373.75

Formula

C17H12ClN3O5

CAS No.
SMILES

O=C(O)CNC(C1=NC=C(C2=CC(C3=CC=CC(Cl)=C3)=NO2)C=C1O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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ZG-2291
Cat. No.:
HY-159120
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