2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. 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.

ZG-2291 Related Antibodies

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.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (133.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6756 mL 13.3779 mL 26.7559 mL
5 mM 0.5351 mL 2.6756 mL 5.3512 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6756 mL 13.3779 mL 26.7559 mL 66.8896 mL
5 mM 0.5351 mL 2.6756 mL 5.3512 mL 13.3779 mL
10 mM 0.2676 mL 1.3378 mL 2.6756 mL 6.6890 mL
15 mM 0.1784 mL 0.8919 mL 1.7837 mL 4.4593 mL
20 mM 0.1338 mL 0.6689 mL 1.3378 mL 3.3445 mL
25 mM 0.1070 mL 0.5351 mL 1.0702 mL 2.6756 mL
30 mM 0.0892 mL 0.4459 mL 0.8919 mL 2.2297 mL
40 mM 0.0669 mL 0.3344 mL 0.6689 mL 1.6722 mL
50 mM 0.0535 mL 0.2676 mL 0.5351 mL 1.3378 mL
60 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
80 mM 0.0334 mL 0.1672 mL 0.3344 mL 0.8361 mL
100 mM 0.0268 mL 0.1338 mL 0.2676 mL 0.6689 mL
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ZG-2291 Related Classifications

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:

ZG-22912962103-40-6ZG2291ZG 2291HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHep3B cellsOb/ob miceAnti-obesity activityMetabolic diseaseInhibitorinhibitorinhibit

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