Triptolide (PG490)

For research use only. Not for use in humans.

目录号:S3604 别名: NSC 163062 中文名称:雷公藤甲素

Triptolide (PG490) Chemical Structure

CAS No. 38748-32-2

Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂,抑制NF-κB转录活性,破坏p65/CBP的相互作用,减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。

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RMB 2060.55 现货
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客户使用Selleck生产的Triptolide (PG490)发表文献27篇:

产品安全说明书

ADC Cytotoxin抑制剂选择性比较

生物活性

产品描述 Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂,抑制NF-κB转录活性,破坏p65/CBP的相互作用,减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。
靶点
NF-κB [1]
()
HSF1 [1]
()
Mdm2 [1]
()
体外研究

Triptolide是一种三环氧二萜类化合物,具有强效的免疫抑制和抗炎性能。在嘌呤盒/核因子和NF-κB介导的转录激活水平,Triptolide能够抑制激活的T细胞中IL-2的表达。[1] Triptolide在极低浓度下(2–10纳克/毫升)能够抑制肿瘤细胞的增殖和集落形成。Triptolide对乳腺癌,胃癌和白血病细胞系HL-60细胞具有抑制活性。在肿瘤细胞中,Triptolide通过阻断NF-κB激活并使肿瘤细胞对TNF-&alpha诱导的程序性细胞死亡敏感来诱导细胞凋亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 MX7DfZRwfG:6aXPpeJkh[WejaX7zeC=> Mk\GR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMtKEmFNUC9NE4xODJzzszN M3HH[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEewPFY1Lz5{MUS3NFg3PDxxYU6=
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SKOV3 NEfrSFRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0 NGnIfZc4OiCqcoO= NF2yWZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wNFbPxE1? Mn3EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6M{O1OFMoRjJyOEOzOVQ{RC:jPh?=
SKOV3 MVnDfZRwfG:6aXPpeJkh[WejaX7zeC=> NEPtXHI4OiCqcoO= MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0xNjByNt88US=> NWO0TnNmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzO|g4ODlpPkK0N|c5PzB7PD;hQi=>
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A549 M{HiZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1 M2\VTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMtKEmFNUC9NE4xOToQvF2= NW\zfGJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0O|A5PjRpPkKxOFcxQDZ2PD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Jun; 

PubMed: 22666381     


(C) and (D) Triptolide decreased c-Jun protein level in LNCaP (C) and PC-3 (D) cells in a dose-dependent manner. Cells were treated with indicated dose of Triptolide or Celastrol for 24 h before Western blot analysis. α-tubulin was used as a loading control. 

MDM2; 

PubMed: 27004407     


Western blot assays showing the dose-response and time-course of MDM2 inhibition by triptolide. GAPDH served as an internal control for equal protein loading.

p-AKT / AKT / p-Foxo3a / Foxo3a / p53 ; 

PubMed: 27004407     


Western blot assays showing the inhibitory effect of triptolide on Akt activity. MCF-7 and MDA-MB-468 cells were treated with 50 nM triptolide for different times. Cell extracts were tested by Western blot assay for the expression of MDM2, p53, p21, PUMA, Akt, phosphorylated Akt (S473), Foxo3a and phosphorylated Foxo3a. Phosphorylated Akt and phosphorylated Foxo3a were dramatically decreased following treatment with triptolide. The quantification results are shown on the graphs to the right. 

p-PI3K / PI3K / p85 / p110 ; 

PubMed: 27004407     


Triptolide up-regulates p85 expression. MDA-MB-468 cells were treated with 50 nM triptolide for different times. Cell extracts were tested by Western blot assay for the expression of PI3K, phosphorylated PI3K, p85, p110 and REST.

22666381 27004407
Growth inhibition assay
Cell viability; 

PubMed: 22666381     


(C) Effect of Triptolide on LNCaP cells. (E) Effect of Triptolide on PC-3 cells.

22666381
体内研究 Triptolide与cyclosporin A协同促进动物模型中移植物的存活,并协同抑制同种异体骨髓移植伴随的移植物抗宿主病。此外,通过抑制c-IAP2 和c-IAP1的诱导作用,它会引起肿瘤细胞的细胞凋亡,同时部分增强肿瘤坏死因子(TNF-α)诱导的细胞凋亡。[1] [3] Triptolide治疗2-3周抑制由四种不同肿瘤细胞系(B16 黑色素瘤,MDA-435 乳腺癌,TSU 膀胱癌,以及MGC80-3 胃癌)形成的异种移植物的生长,表明TPL具有广谱的抗肿瘤活性,对野生型和突变体p53均具有作用。此外,在实验中,Triptolide抑制B16F10细胞转移到小鼠的肺和脾脏中。[2] 在小鼠模型中,Triptolide在体内外均具有抗多囊性肾病的作用。[4] LD50: 小鼠0.83毫克/千克(静脉注射)。 [5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 72 mg/mL warmed (199.77 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
3mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 360.4
化学式

C20H24O6

CAS号 38748-32-2
储存条件 粉状
溶于溶剂
别名 NSC 163062

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

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