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Methyl Gerfelin

Names

[ CAS No. ]:
700870-56-0

[ Name ]:
Methyl Gerfelin

[Synonym ]:
Gerfelin methyl
MGI
2za0
Methyl Gerfelin

Biological Activity

[Description]:

Methyl gerfelin inhibits osteoclast differentiation by binding 3 major cellular proteins: glyoxalase 1 (GLO1), sterol binding protein 2 (SCP2), and small glutamine-rich tetratricopeptide repeat containing protein A (SGTA). Methyl gerfelin is a potent GLO1 inhibitor related to the flavonoid class[1][2].

[Related Catalog]:

Research Areas >> Others

[Target]

Glyoxalase 1 (GLO1), Sterol binding protein 2 (SCP2), Small glutamine-rich tetratricopeptide repeat containing protein A (SGTA)[1]


[In Vitro]

Methyl gerfelin (0-30 μM; 72 h) 抑制破骨细胞形成，IC50 为 2.8 μM，有效浓度下不影响成熟破骨细胞存活和功能[1]。

[References]

[1]. Kanoh N, et al. Dual structure-activity relationship of osteoclastogenesis inhibitor methyl gerfelin based on TEG scanning. Bioconjug Chem. 2013 Jan 16;24(1):44-52.  

[2]. Perez C, et al. Metal-Binding Pharmacophore Library Yields the Discovery of a Glyoxalase 1 Inhibitor. J Med Chem. 2019 Feb 14;62(3):1609-1625.  

Chemical & Physical Properties

[ Molecular Formula ]:
C16H16O6

[ Molecular Weight ]:
304.29500

[ Exact Mass ]:
304.09500

[ PSA ]:
96.22000

[ LogP ]:
2.99910

Related Compounds