Triptonide(Synonyms: 雷公藤内酯酮; NSC 165677; PG 492)

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Triptonide (Synonyms: 雷公藤内酯酮; NSC 165677; PG 492) 纯度: 99.73%

Triptonide (NSC 165677) 是从雷公藤中鉴定出的一种天然产物。Triptonide 是一种 Wnt 信号抑制剂，其 IC50 约为 0.3 nM。Triptonide 具有免疫抑制、抗炎、避育、神经保护和抗淋巴瘤作用。

Triptonide(Synonyms: 雷公藤内酯酮; NSC 165677; PG 492)

Triptonide Chemical Structure

CAS No. : 38647-11-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2251 In-stock
10 mg ￥2046 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects[1][2].

IC50 & Target

IC50: 0.3 nM (Wnt)[1]
体外研究
(In Vitro)

Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells[1].
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively[2].
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability[2].
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells[2].
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: B-lymphoma Raji cells, T-lymphoma Jurkat cells
Concentration: 0-80 nM
Incubation Time: 3 days, 6 days
Result: Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner.

Apoptosis Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM).

Western Blot Analysis[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels.

RT-PCR[2]

Cell Line: Raji cells
Concentration: 5 nM, 10 nM
Incubation Time: 72 hours
Result: Significantly diminished Lyn mRNA levels in the lymphoma cells.

体内研究
(In Vivo)

Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 107 Raji cells xenograft[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, daily, for 34 days
Result: Potently inhibited lymphoma cell growth and tumorigenic capability.

分子量

358.39

Formula

C20H22O6
CAS 号

38647-11-9
中文名称

雷公藤内酯酮；雷藤酮；雷公藤羰内酯
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

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

    [2]. Ping Yang, et al. Triptonide acts as a novel potent anti-lymphoma agent with low toxicity mainly through inhibition of proto-oncogene Lyn transcription and suppression of Lyn signal pathway. Toxicol LettPing Yang. 2017 Aug 15;278:9-17.

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