1. Immunology/Inflammation Cell Cycle/DNA Damage Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis MAPK/ERK Pathway NF-κB
  2. Akt Interleukin Related NF-κB p38 MAPK CDK NOD-like Receptor (NLR) Caspase Apoptosis Cytochrome P450 PI3K
  3. Tabersonine

Tabersonine  (Synonyms: 水甘草碱)

目录号: HY-N1431 纯度: 98.14%
COA 产品使用指南 技术支持

Tabersonine 是一种选择性、口服有效的 NLRP3 抑制剂。Tabersonine 直接结合 NLRP3 的 NACHT 结构域,抑制其 ATP 酶活性及寡聚化,进而阻断 ASC 斑点形成和 caspase-1 激活,减少 IL-1β 等促炎细胞因子释放。Tabersonine 同时抑制 TRAF6 的 K63 连接泛素化,阻断 NF-κBPI3K/Aktp38 MAPK 信号通路。Tabersonine 可抑制炎症反应,通过线粒体通路和死亡受体通路诱导肝癌细胞凋亡 (apoptosis),降低线粒体膜电位、促进细胞色素 c 释放并激活 caspase 蛋白。Tabersonine 主要用于 NLRP3 驱动的炎症性疾病 (如急性肺损伤、败血症、腹膜炎) 及肝癌等肿瘤的研究。

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Tabersonine

Tabersonine Chemical Structure

CAS No. : 4429-63-4

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10 mM * 1 mL in DMSO ¥414
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1 mg ¥248
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5 mg ¥560
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10 mg ¥810
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25 mg ¥1338
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50 mg ¥1975
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100 mg ¥2940
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Customer Review

Other Forms of Tabersonine:

IHC

    Tabersonine purchased from MCE. Usage Cited in: Phytother Res. 2023 Jun;37(6):2353-2363.  [Abstract]

    Tabersonine (Tab; 20 mg/kg; i.v; every 2 days for 12 weeks) significantly reduces the expression and transcription of these fibrotic related biomarkers (mRNA levels of Col1a1, Tgfb1, and Acta2, protein levels of COL-1 and TGF-β) in C57BL/6 mice.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer[1][2][3].

    IC50 & Target

    CDK4

     

    IL-1β

     

    Caspase-1

     

    Caspase-8

     

    NLRP3

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    14.7 μM
    Compound: 12
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 22260257]
    HL-60 IC50
    4.5 μM
    Compound: 12
    Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
    Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
    [PMID: 22260257]
    MCF7 IC50
    9.9 μM
    Compound: 12
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 22260257]
    SMMC-7721 IC50
    5.6 μM
    Compound: 12
    Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay
    Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay
    [PMID: 22260257]
    SW480 IC50
    12.1 μM
    Compound: 12
    Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
    Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
    [PMID: 22260257]
    体外研究
    (In Vitro)

    Tabersonine (0.78-25 μM;24 h) 可抑制人肝癌细胞 SMMC-7721、HepG2 和人正常肝细胞 HL-7702 的细胞活力,且对肝癌细胞的抑制作用更强[1]
    Tabersonine (6.25-25 μM;24 h) 能诱导人肝癌细胞 SMMC-7721 凋亡,上调 Bax、cleaved-caspase-3、cleaved-PARP 蛋白表达,下调 Bcl-2 蛋白表达[1]
    Tabersonine (12.5-25 μM;24 h) 将 SMMC-7721 细胞周期阻滞于 G0/G1 期,下调 CDK4、Cyclin D1 蛋白表达[1]
    Tabersonine (25 μM;6 h、12 h、24 h) 能抑制 SMMC-7721 细胞中 NLRP3、ASC、cleaved-caspase-1、IL-1β 的 mRNA 和蛋白表达[1]
    Tabersonine (6-30 μM;18 h) 诱导 HepG2 细胞凋亡,造成线粒体功能损伤,和 PI3K/Akt 通路抑制[2]
    Tabersonine 抑制 BMDM 细胞中 NLRP3 介导的 IL-1β 生成的 IC50 为 0.71 μM[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: SMMC-7721, HepG2, HL-7702
    Concentration: 0.78 μM, 1.56 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM
    Incubation Time: 24 h
    Result: Inhibited the cell viability of SMMC-7721, HepG2 and HL-7702 cells. The inhibitory effect on SMMC-7721 and HepG2 cells was stronger than that on HL-7702 cells, indicating a certain degree of selectivity for tumor cells.

    Apoptosis Analysis[1]

    Cell Line: SMMC-7721
    Concentration: 6.25 μM, 12.5 μM, 25 μM
    Incubation Time: 24 h
    Result: Induced apoptosis in SMMC-7721 cells.
    The protein expression of Bax, cleaved-caspase-3 and cleaved-PARP was up-regulated, while the protein expression of Bcl-2 was down-regulated.
    体内研究
    (In Vivo)

    Tabersonine (10-40 mg/kg;腹腔注射;每日 1 次;30 天) 在小鼠 LPS 诱导急性肺损伤模型中,减轻肺组织病理损伤,抑制中性粒细胞浸润、降低 MPO 活性及 TNF-α、IL-6、IL-1β 水平[1]
    Tabersonine (25、50 mg/kg;灌胃;每日 1 次;3 周) 在裸鼠 HepG2 肝癌移植瘤模型中,显著抑制肿瘤生长,诱导肿瘤组织中裂解的 Caspase-3 表达并促进细胞凋亡[2]
    Tabersonine (10 mg/kg;灌胃;每日 3 次;连续处理) 在小鼠 LPS 诱导急性肺损伤及 Alum 诱导腹膜炎模型中,抑制 NLRP3 炎症小体激活,减少 IL-1β 释放及炎症细胞浸润;在大肠杆菌诱导的败血症模型中,提升小鼠 48 h 生存率至60%[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male C57BL/6 mice (25-30 g, 8-10 weeks old), LPS-induced acute lung injury model[1]
    Dosage: 10, 20, 40 mg/kg
    Administration: Intraperitoneal injection, daily for 30 days
    Result: Significantly alleviated pathological injury in lung tissues, inhibited neutrophil infiltration, reduced myeloperoxidase (MPO) activity, and decreased the levels of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β compared to the LPS control group.
    分子量

    336.43

    Formula

    C21H24N2O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    水甘草碱

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 25 mg/mL (74.31 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9724 mL 14.8619 mL 29.7239 mL
    5 mM 0.5945 mL 2.9724 mL 5.9448 mL
    查看完整储备液配制表

    * 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 (protect from light)。-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。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 98.14%

    参考文献

    完整储备液配制表

    * 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 (protect from light)。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9724 mL 14.8619 mL 29.7239 mL 74.3097 mL
    5 mM 0.5945 mL 2.9724 mL 5.9448 mL 14.8619 mL
    10 mM 0.2972 mL 1.4862 mL 2.9724 mL 7.4310 mL
    15 mM 0.1982 mL 0.9908 mL 1.9816 mL 4.9540 mL
    20 mM 0.1486 mL 0.7431 mL 1.4862 mL 3.7155 mL
    25 mM 0.1189 mL 0.5945 mL 1.1890 mL 2.9724 mL
    30 mM 0.0991 mL 0.4954 mL 0.9908 mL 2.4770 mL
    40 mM 0.0743 mL 0.3715 mL 0.7431 mL 1.8577 mL
    50 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
    60 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2385 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
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