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Parthenolide

Parthenolide

产品编号 T2140   CAS 20554-84-1
别名: (-)-Parthenolide, 小白菊内酯

Parthenolide ((-)-Parthenolide) 是一种从药草短舌匹菊中发现的倍半萜内酯。 它抑制NF-κB 活化,有抗炎活性。它还可抑制HDAC1蛋白,但不影响其他I/II 类HDAC

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Parthenolide Chemical Structure
Parthenolide, CAS 20554-84-1
规格 价格/CNY 货期 数量
25 mg ¥ 298 现货
50 mg ¥ 418 现货
100 mg ¥ 587 现货
200 mg ¥ 925 现货
500 mg ¥ 1,569 现货
1 mL * 10 mM (in DMSO) ¥ 270 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Parthenolide (T2140)
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纯度: 99.46%
纯度: 99.33%
纯度: 99.10%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
TCMIP信息
参考文献
植物来源
结构类型
产品描述 (-)-Parthenolide ((-)-Parthenolide), an inhibitor of the Nuclear Factor-κB Pathway, also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
体外活性 Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells which indicates that apoptosis is trigged after Parthenolide exposure. Besides induction of apoptosis, Parthenolide also induces G0/G1 cell cycle arrest in a concentration-dependent manner in A549 cells and G2/M cell cycle arrest in H1792 cells[2].
体内活性 Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect in Phb1 KO hepatocytes. Actually, TSA and Parthenolide-treated hepatocytes exhibited increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a result of specific HDAC inhibition, resulting in the attenuation of the Phb1 KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL in Phb1 KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to control Phb1 KO mice[3].
细胞实验 Parthenolide (PTL) is dissolved in DMSO and diluted with appropriate media[2]. Cells are seeded in 96-well plates and treated on the second day with the given concentration of Parthenolide (0, 5, 10, 20 μM) for another 48 hours and then subjected to SRB or MTT assay. For SRB assay, live cell number is estimated as described earlier. After treatment, the medium is discarded firstly. In order to fix the adherent cells, 100 μL of cold trichloroacetic acid (10% (w/v)) are adding to each well and incubating at 4°C for at least 1 hour. The plates are then washed five times with deionized water and dried in the air. Each well are then added with 50 μL of SRB solution (0.4% w/v in 1% acetic acid) and incubated for 5 min at room temperature. The plates are washed five times with 1% acetic acid to remove unbound SRB and then air dried. The residual bound SRB is solubilized with 100 μL of 10 mM Tris base buffer (pH 10.5), and then read using a microtiter plate reader at 495 nm. The MTT assay is executed. 20 μL MTT (5 mg/mL) are added to each sample and incubate at 37°C for 4 h, then 100 μL solubilization solution are added. Cell viability is determined at 595 nm[2].
别名 (-)-Parthenolide, 小白菊内酯
分子量 248.32
分子式 C15H20O3
CAS No. 20554-84-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 49 mg/mL (197.33 mM)

Ethanol: 50 mg/mL (201.35 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 4.0271 mL 20.1353 mL 40.2706 mL 100.6765 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL 20.1353 mL
10 mM 0.4027 mL 2.0135 mL 4.0271 mL 10.0677 mL
20 mM 0.2014 mL 1.0068 mL 2.0135 mL 5.0338 mL
50 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0135 mL
100 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
TCMIP相关数据
中药材来源及性味归经
所属中成药

中药材来源及性味归经

中药材名称 中药材拉丁名 归经
长叶天名精 Carpesium longifolium Chen et C. M. Hu -
黄缅桂 Michelia champaca L.
雷公藤 Tripterygium wilfordii Hook. f. 辛, 苦 心, 肝
云南含笑 Michelia yunnanensis Franch. ex Finet et Gagnep. -
皱叶木兰 Magnolia praecocissima Koidz. -

所属中成药

中成药名称 处方组成 主治疾病 中成药类型
雷公藤片 雷公藤 N/A 清热药
金关片 雷公藤,续断,山药,细辛,制附子,茯苓,桑枝,桂枝,鹿角霜,秦艽,丹参,枸杞子,牛膝,鸡血藤,黄精,淫羊藿,薏苡仁,黄芪 口服,一次4片,一日3次。 扶正药

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TargetMol Library Books参考文献

1. Nakshatri, H., Appaiah, H., Anjanappa, M., Gilley, D., Tanaka, H., & Badve, S. et al. (2015). NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT. Cell Death & Disease, 6(1), e1608-e1608. doi: 10.1038/cddis.2014.569 2. Zhao X, et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33:3. 3. Barbier-Torres L, et al. Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1. Hepatology. 2015 Oct;62(4):1237-48.
Chetomin Ethylene dimethanesulfonate Nerol 2-Deoxy-D-glucose Orlistat Pyroxamide Minodronic acid EI1

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌临床化合物库 药物功能重定位化合物库 抗癌药物库 染色质修饰分子库 泛素化化合物库 萜类天然产物库 转录因子库 铁死亡化合物库 细胞凋亡化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Parthenolide 20554-84-1 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair NF-Κb Mitophagy NF-κB HDAC inhibit (-)-Parthenolide Nuclear factor-kappaB Mitochondrial Autophagy Nuclear factor-κB 小白菊内酯 Inhibitor inhibitor

 

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