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522-17-8

中文名稱 魚藤素
英文名稱 DEGUELIN
CAS 522-17-8
分子式 C23H22O6
分子量 394.42
MOL 文件 522-17-8.mol
更新日期 2024/12/16 08:26:33
522-17-8 結(jié)構(gòu)式 522-17-8 結(jié)構(gòu)式

基本信息

中文別名
藤素
魚藤素
(-)-DEGUELIN
AKT抑制劑(DEGUELIN)
英文別名
DEGUELIN
Ccris 8104
()-Deguelin
(-)-DEGUELIN
(7as-cis)-oxy-
Deguelin (6CI)
(-)-cis-Deguelin
12a-DEOXYTEPHROSIN
(-)-DEGUELIN
(-)-CIS-DEGUELIN
3h-bis(1)benzopyrano(3,4-b:6’,5’-e)pyran-7(7ah)-one,13,13a-dihydro-9,10-dimeth
所屬類別
天然產(chǎn)物:黃酮類化合物

物理化學(xué)性質(zhì)

熔點85-87 °C(lit.)
比旋光度D27 -97.2° (c = 0.2 in benzene)
沸點560.1±50.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
儲存條件-20°C
溶解度DMSO: >10 mg/mL
形態(tài)solid
顏色white to yellow
旋光性 (optical activity)[α]/D -70 to -80°, c = 0.2 in methanol
穩(wěn)定性從購買之日起 2 年內(nèi)保持穩(wěn)定。 DMSO 或乙醇溶液可在 -20℃ 下保存長達(dá) 3 個月。

安全數(shù)據(jù)

安全說明22-24/25
WGK Germany3
RTECS號DX1500000
海關(guān)編碼29329990
魚藤素價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-13425魚藤素
Deguelin
522-17-85mg424元
2024/11/08HY-13425魚藤素
Deguelin
522-17-810mM * 1mLin DMSO542元
2024/11/08HY-13425魚藤素
Deguelin
522-17-810mg784元

常見問題列表

生物活性
Deguelin 是一種天然存在的魚藤酮類化合物,通過阻止多種途徑 (如 PI3K-Akt,IKK-NF-κB 和 MAPK-mTOR-survivin 等) 充當(dāng)化學(xué)預(yù)防劑。Deguelin 與 Hsp90 的結(jié)合導(dǎo)致許多致癌蛋白 (包括 MEK1/2,Akt,HIF1α,COX-2 和 NF-κB) 的表達(dá)降低。。
靶點

Akt

體外研究

Deguelin (0-500 nM) in a dose and time dependent manner inhibits the growth of MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin at all concentrations fails to reduce cell numbers in the presence of 1 ng EGF but in the presence of EGF 20 ng reinstated deguelin mediated growth inhibition. Deguelin treated cells show reduced expression of Survivin as determined by western blot and immunofluorescence examinations. Deguelin inhibits p-ERK and its downstream target p-STAT-3 and c-Myc expression in a dose dependent manner. Deguelin down-regulates Akt signaling probably by disrupting its association with Hsp 90 in cultured HNSCC cells. Deguelin deguelin disrupts the association between Hsp 90 with survivin and Cdk4. Deguelin deguelin treatment increases cellular ceramide level through de novo synthase pathway to mediate HNSCC cell death and apoptosis. Deguelin inhibits the proliferation of MPC-11 cells in a concentration- and time-dependent manner and causes the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt is decreased. Deguelin-induced apoptosis is characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3.

體內(nèi)研究

Deguelin (2 or 4 mg/kg, i.p.) reduces the in vivo tumor growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice. Deguelin (4 mg/kg, p.o.) treatment shows a great inhibition in tumor growth, which is demonstrated by reduced tumor size and improved mice survival and, indicating a significant anti-tumor ability by deguelin in vivo. In the colon cancer xenograft model, the volume of the tumor treated with deguelin is significantly lower than that of the control, and the apoptotic index for deguelin-treated mice is much higher.

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