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Triptonide

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Chemical Structure| 38647-11-9 同义名 : PG 492;NSC 165677;(−)-Triptonide
CAS号 : 38647-11-9
货号 : A224906
分子式 : C20H22O6
纯度 : 99%+
分子量 : 358.385
MDL号 : MFCD00210566
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(292.98 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Triptonide, a natural product isolated and purified from the herb of Tripterygium wilfordii Hook.f. with antileukemic, antitumor, anti-inflammatory activities, is effective in the treatment of autoimmune diseases. Triptonide can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. In addition, triptonide treatment robustly rescued the zebrafish "eyeless" phenotype induced by GSK-3β antagonist 6-bromoindirubin-30-oxime (BIO) for Wnt signaling activation during embryonic gastrulation[3]. Triptonide effectively suppressed TNBC (Triple-negative breast cancer) cell tumorigenesis, vasculogenic mimicry, and strongly inhibited the metastasis of TNBC via degradation of Twist1 and Notch1 oncoproteins, downregulation of metastatic and angiogenic gene expression, and reduction of NF-κB signaling pathway[4]. Single daily oral doses of triptonide induces deformed sperm with minimal or no forward motility (close to 100% penetrance) and consequently male infertility in 3-4 and 5-6 weeks in mice and cynomolgus monkeys, respectively[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.40mL

27.90mL

5.58mL

2.79mL

参考文献

[1]Chinison J, Aguilar JS, et al. Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin. Sci Rep. 2016 Sep 6;6:32779.

[2]Ning L, Qu G, et al. Cytotoxic biotransformed products from triptonide by Aspergillus niger. Planta Med. 2003 Sep;69(9):804-8.

[3]Chinison J, Aguilar JS, Avalos A, Huang Y, Wang Z, Cameron DJ, Hao J. Triptonide Effectively Inhibits Wnt/β-Catenin Signaling via C-terminal Transactivation Domain of β-catenin. Sci Rep. 2016 Sep 6;6:32779

[4]Zhang M, Meng M, Liu Y, Qi J, Zhao Z, Qiao Y, Hu Y, Lu W, Zhou Z, Xu P, Zhou Q. Triptonide effectively inhibits triple-negative breast cancer metastasis through concurrent degradation of Twist1 and Notch1 oncoproteins. Breast Cancer Res. 2021 Dec 18;23(1):116

[5]Chang Z, Qin W, Zheng H, Schegg K, Han L, Liu X, Wang Y, Wang Z, McSwiggin H, Peng H, Yuan S, Wu J, Wang Y, Zhu S, Jiang Y, Nie H, Tang Y, Zhou Y, Hitchcock MJM, Tang Y, Yan W. Triptonide is a reversible non-hormonal male contraceptive agent in mice and non-human primates. Nat Commun. 2021 Feb 23;12(1):1253