<Suppliers Price>

Glabrescione B

Names

[ CAS No. ]:
65893-94-9

[ Name ]:
Glabrescione B

[Synonym ]:
3-[3,4-bis-(3-methyl-but-2-enyloxy)-phenyl]-5,7-dimethoxy-chromen-4-one
Glabrescion B
3-[3,4-Bis-(3-methyl-but-2-enyloxy)-phenyl]-5,7-dimethoxy-chromen-4-one
3-(3',4'-bis(3-methylbut-2-enyloxy)phenyl)-5,7-dimethoxy-4H-chromen-4-one

Biological Activity

[Description]:

Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells[1][2].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Gli
Research Areas >> Cancer

[Target]

Gli1-DNA Interaction[1]


[In Vitro]

Glabrescione B (5 μM; 24-72 hours) inhibits the growth of Gli-dependent basal cell carcinoma[2]. Glabrescione B (1-10 μM; 24-48 hours) decreases Gli1 mRNA expression levels[2]. Cell Proliferation Assay[1] Cell Line: ASZ001 BCC cells Concentration: 5 μM Incubation Time: 24-72 hours Result: Basal cell carcinoma cell proliferation was impaired. Western Blot Analysis[1] Cell Line: ASZ001 BCC cells Concentration: 1-10 μM Incubation Time: 24-48 hours Result: Gli1 mRNA expression levels was decreased.

[In Vivo]

Animal Model: Female NOD/SCID mice (ASZ001 BCC allografts)[2] Dosage: 100 μmol/kg Administration: I.p.; every second day for 18 days Result: A significant reduction of tumor growth as well as Gli1 mRNA levels was observed.

[References]

[1]. Ingallina C, et al. Polymeric glabrescione B nanocapsules for passive targeting of Hedgehog-dependent tumor therapy in vitro. Nanomedicine (Lond). 2017;12(7):711-728.

[2]. Infante P, et al. Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors. EMBO J. 2015;34(2):200-217.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H30O6

[ Molecular Weight ]:
450.52400

[ Exact Mass ]:
450.20400

[ PSA ]:
67.13000

[ LogP ]:
6.16720

Related Compounds