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

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.

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CAS 番号 : 4429-63-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 31 在庫あり
Solution
10 mM * 1 mL in DMSO USD 31 在庫あり
Solid
10 mg $29 在庫あり
25 mg $59 在庫あり
50 mg $89 在庫あり
100 mg $134 在庫あり
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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Tabersonine:

Tabersonine 関連抗体

Top Publications Citing Use of Products

    Tabersonine purchased from MedChemExpress. 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.

    Akt アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Akt Akt1 Akt2 Akt3

    Interleukin Related アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

    NF-κB アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    p38 MAPK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

    CDK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NLRP3 NLRP1 NOD1 NOD2

    Caspase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    Cytochrome P450 アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

    PI3K アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    18 μM
    Compound: Tab
    Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured after 48 hrs by CCK8 assay
    		[PMID: 38417401]
    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]
    MDA-MB-231 IC50
    5.59 μM
    Compound: 3; TAB
    Antiproliferative activity against human MDA-MB-231 cells
    Antiproliferative activity against human MDA-MB-231 cells
    		[PMID: 37122543]
    SK-OV-3 IC50
    25 μM
    Compound: Tab
    Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured after 48 hrs by CCK8 assay
    		[PMID: 38417401]
    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]
    体外実験

    Tabersonine (0.78-25 μM; 24 h) inhibits the cell viability of human liver cancer cells SMMC-7721, HepG2 and human normal liver cells HL-7702, with a stronger inhibitory effect on liver cancer cells[1].
    Tabersonine (6.25-25 μM; 24 h) induces apoptosis of human liver cancer cells SMMC-7721, upregulates the expression of Bax, cleaved-caspase-3, and cleaved-PARP proteins, and downregulates the expression of Bcl-2 protein[1].
    Tabersonine (12.5-25 μM; 24 h) arrests the cell cycle of SMMC-7721 cells at the G0/G1 phase, and downregulates the expression of CDK4 and Cyclin D1 proteins[1].
    Tabersonine (25 μM; 6 h, 12 h, 24 h) inhibits the mRNA and protein expressions of NLRP3, ASC, cleaved-caspase-1, and IL-1β in SMMC-7721 cells[1].
    Tabersonine (6-30 μM; 18 h) induces apoptosis in HepG2 cells, resulting in mitochondrial function impairment, and PI3K/Akt pathway inhibition[2].
    Tabersonine inhibits NLRP3-mediated IL-1β production in BMDM cells with an IC50 of 0.71 μM[3].

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

    Tabersonine 関連抗体

    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.
    体内実験

    Tabersonine (10-40 mg/kg; intraperitoneal injection; once a day; 30 days) reduces lung tissue pathological damage, inhibits neutrophil infiltration, reduces MPO activity and TNF-α, IL-6, and IL-1β levels in the mouse LPS-induced acute lung injury model[1].
    Tabersonine (25, 50 mg/kg; oral gavage; once a day; 3 weeks) significantly inhibits tumor growth in the nude mouse HepG2 liver cancer xenograft model, induces the expression of cleaved Caspase-3 in tumor tissues and promotes cell apoptosis[2].
    Tabersonine (10 mg/kg; gavage; 3 times a day; 48-120 h) inhibits NLRP3 inflammasome activation, reduces IL-1β release and inflammatory cell infiltration in the mouse LPS-induced acute lung injury and Alum-induced peritonitis models; and increases the 48-hour survival rate of mice to 60% in the Escherichia coli-induced sepsis model[3].

    MedChemExpress (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

    分子式

    C21H24N2O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(OC)C1=C2NC3=CC=CC=C3[C@@]24CCN5CC=C[C@@]([C@@]45[H])(CC)C1
    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light

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

    DMSO : 25 mg/mL (74.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2972 mL 1.4862 mL 2.9724 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    純度とドキュメンテーション

    純度: 98.13%

    COA (254 KB) HNMR (257 KB) LCMS (345 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
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    Tabersonine Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • 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.

    Keywords:

    Tabersonine4429-63-4AktInterleukin RelatedNF-κBp38 MAPKCDKNOD-like Receptor (NLR)CaspaseApoptosisCytochrome P450PI3KPKBProtein kinase BILNuclear factor-κBNuclear factor-kappaBCyclin dependent kinaseCYPsPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-N1431
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