65893-94-9
中文名稱
GLABRESCIONE B
英文名稱
Glabrescione B
CAS
65893-94-9
分子式
C27H30O6
分子量
450.52
MOL 文件
65893-94-9.mol
65893-94-9 結(jié)構(gòu)式
基本信息
英文別名
GlaBGlabrescione B
Glabrescione B (GlaB)
3-[3,4-bis-(3-methyl-but-2-enyloxy)-phenyl]-5,7-dimethoxy-chromen-4-one
4H-1-Benzopyran-4-one, 3-[3,4-bis[(3-methyl-2-buten-1-yl)oxy]phenyl]-5,7-dimethoxy-
物理化學(xué)性質(zhì)
沸點(diǎn)608.0±55.0 °C(Predicted)
密度1.142±0.06 g/cm3(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
Glabrescione B 是第一個(gè)結(jié)合 Hedgehog (Hh) 調(diào)節(jié)劑 Gli1 并通過干擾 Gli1-DNA 相互作用而削弱其活性的化合物。Glabrescione B 抑制 Hedgehog 依賴性腫瘤細(xì)胞的生長(zhǎng)，抑制腫瘤源性干細(xì)胞的自我更新能力和克隆能力。靶點(diǎn)
Gli1-DNA Interaction
體外研究
Glabrescione B (5 μM; 24-72 hours) inhibits the growth of Gli-dependent basal cell carcinoma.
Glabrescione B (1-10 μM; 24-48 hours) decreases Gli1 mRNA expression levels.
Cell Proliferation Assay
| Cell Line: | ASZ001 BCC cells |
| Concentration: | 5 μM |
| Incubation Time: | 24-72 hours |
| Result: | Basal cell carcinoma cell proliferation was impaired. |
Western Blot Analysis
| Cell Line: | ASZ001 BCC cells |
| Concentration: | 1-10 μM |
| Incubation Time: | 24-48 hours |
| Result: | Gli1 mRNA expression levels was decreased. |
體內(nèi)研究
| Animal Model: | Female NOD/SCID mice (ASZ001 BCC allografts) |
| 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. |