Emodin  (Synonyms: Frangula emodin)

Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction^[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects^[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice^[3].

Emodin (10-400 μM) blocks the binding of S protein to ACE2 in a dose-dependent manner with the IC₅₀ value of 200 μM^[1].
Emodin (5-50 μM) inhibits the S protein-pseudotyped retrovirus infectivity in a dose-dependent manner. Emodin blocks the SARS-CoV S protein binding to Vero E6 cells^[1].
Emodin inhibits casein kinase-2 (CK2) with IC₅₀s of 5.9, 30.0, and 7.1 μM for CK2α Wild-type, Ile174Ala mutant, and His160Ala mutant at ATP concentration is 50 μM, respectively. The IC₅₀s are 1.40 and 38.00 μM for CK2α Wild-type, and Val66Ala mutant at ATP concentration is 10 μM^[2].
Emodin exhibits low inhibitory activity against mouse and human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), with an IC₅₀ higher than 1 mM, indicating that Emodin is more than 5000-fold selective for the human and mouse 11β-HSD1 enzymes over the type 2 isoenzyme^[3].

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

Emodin (single oral administration of 100 or 200 mg/kg) inhibits 11β-HSD1 activity in normal C57BL/6J male mice^[3].
Emodin (100 mg/kg; oral administration; b.i.d.) improves insulin sensitivity and lipid metabolism, and lowers blood glucose and hepatic PEPCK, and glucose-6-phosphatase mRNA in diet-induced obese (DIO) mice^[3].

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

270.24

C₁₅H₁₀O₅

518-82-1

Solid

Yellow to orange

O=C1C2=C(C=C(C)C=C2O)C(C3=CC(O)=CC(O)=C31)=O

Room temperature in continental US; may vary elsewhere.

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

• [1]. Tin-Yun Ho, et al. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction. Antiviral Res. 2007 May;74(2):92-101.  [Content Brief]

  [2]. Stefania Sarno, et al. Toward the rational design of protein kinase casein kinase-2 inhibitors. Pharmacol Ther. Feb-Mar 2002;93(2-3):159-68.  [Content Brief]

  [3]. Ying Feng, et al. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26.  [Content Brief]