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

Tabersonine hydrochloride  (Synonyms: 水甘草碱盐酸盐)

目录号: HY-N1431A
产品使用指南 技术支持

Tabersonine hydrochloride 是一种选择性、口服有效的 NLRP3 抑制剂。Tabersonine hydrochloride 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 hydrochloride 同时抑制 TRAF6 的 K63 连接泛素化，阻断 NF-κB、PI3K/Akt、p38 MAPK 信号通路。Tabersonine hydrochloride 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 hydrochloride 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 hydrochloride

Tabersonine hydrochloride Chemical Structure

CAS No. : 29479-00-3

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Other Forms of Tabersonine hydrochloride:

Tabersonine hydrochloride 相关抗体

Top Publications Citing Use of Products

    Tabersonine hydrochloride 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.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride 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 hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride 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 hydrochloride 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

     

    体外研究
    (In Vitro)

    Tabersonine hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride 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.

    Tabersonine hydrochloride 相关抗体:

    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) hydrochloride 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) hydrochloride 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) hydrochloride 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 Tabersonine
    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

    372.89

    Formula

    C21H25ClN2O2
    CAS 号
    中文名称

    水甘草碱盐酸盐
    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Tabersonine hydrochloride 相关分类

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    Keywords:

    Tabersonine29479-00-3水甘草碱盐酸盐AktInterleukin RelatedNF-κBp38 MAPKCDKNOD-like Receptor (NLR)CaspaseApoptosisCytochrome P450PI3KPKBProtein kinase BILNuclear factor-κBNuclear factor-kappaBCyclin dependent kinaseCYPsPhosphoinositide 3-kinaseAβ(1-42)LI/ARDSInhibitorinhibitorinhibit

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