Glabrescione B|GlaB|CAS 65893-94-9|DC Chemicals

Cas No.:	65893-94-9
Chemical Name:	3-[3,4-bis(3-methylbut-2-enoxy)phenyl]-5,7-dimethoxychromen-4-one
Synonyms:	GlaB
SMILES:	O=C1C(C2=CC=C(OC/C=C(C)/C)C(OC/C=C(C)/C)=C2)=COC3=CC(OC)=CC(OC)=C13
Formula:	C₂₇H₃₀O₆
M.Wt:	450.52
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1. Infante P, et al. EMBO J. 2015 Jan 13;34(2):200-17. 2. Ingallina C, et al. Nanomedicine (Lond). 2017 Apr;12(7):711-728.

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].
Target:	Gli1-DNA Interaction[1]
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.
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.
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.

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