1. Apoptosis PI3K/Akt/mTOR NF-κB Stem Cell/Wnt TGF-beta/Smad JAK/STAT Signaling Epigenetics Protein Tyrosine Kinase/RTK Anti-infection
  2. IAP Akt Caspase NF-κB TGF-beta/Smad JAK Bacterial Apoptosis
  3. Jolkinolide B

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis.

For research use only. We do not sell to patients.

CAS No. : 37905-08-1

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Jolkinolide B:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Jolkinolide B

Cell Proliferation/Viability Assay
Cell Migration/Invasion Assay
WB
Apoptosis Analysis
RT-PCR

    Jolkinolide B purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Apr 17;19(4):e0299920.  [Abstract]

    Cell viability assays of Huh-7, SK-Hep-1 and L-02 cells were performed using CCK-8 method after treatment with different concentrations (0, 5, 10, 25, 50, or 100 μM) of Jolkinolide B for 48 h.

    Jolkinolide B purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Apr 17;19(4):e0299920.  [Abstract]

    Huh-7 and SK-Hep-1 cells were seeded, scratched, and then treated with Jolkinolide B at a concentration of 10 μM for 48 h. The wound healing assays were performed to assess the migration abilities of Huh-7 and SK-Hep-1 cells.

    Jolkinolide B purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Apr 17;19(4):e0299920.  [Abstract]

    Huh-7 and SK-Hep-1 cells were treated with DMSO or Jolkinolide B at a concentration of 10 μM for 48 h; then the protein expression of E-cadherin and vimentin was analyzed using western blotting.

    Jolkinolide B purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Apr 17;19(4):e0299920.  [Abstract]

    Huh-7 and SK-Hep-1 cells were treated with DMSO or Jolkinolide B, the cells apoptosis was analyzed by flow cytometry and apoptosis rates were calculated.

    Jolkinolide B purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Apr 17;19(4):e0299920.  [Abstract]

    Huh-7 and SK-Hep-1 cells were treated with 10 μM Jolkinolide B for 48 h. The mRNA expression of MMP-7 and C-MYC in Huh-7 and SK-Hep-1 cells analyzed using RT-qPCR method.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis[1][2][3][4].

    IC50 & Target[1][3]

    Akt

     

    cIAP-1

     

    cIAP-2

     

    XIAP

     

    Caspase-9

     

    Caspase-3

     

    NFκB

     

    JAK

     

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    5.09 μg/mL
    Compound: 8
    Cytotoxicity against human A2780 cells by MTT assay
    Cytotoxicity against human A2780 cells by MTT assay
    [PMID: 18205316]
    A549 IC50
    28.238 μM
    Compound: Compound 4
    Cytotoxicity against human A549 cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human A549 cells assessed as cell growth inhibition by MTT assay
    [PMID: 27913179]
    A549 IC50
    6.1 μg/mL
    Compound: 8
    Cytotoxicity against human A549 cells by MTT assay
    Cytotoxicity against human A549 cells by MTT assay
    [PMID: 18205316]
    BGC-823 IC50
    5.81 μg/mL
    Compound: 8
    Cytotoxicity against human BGC 823 cells by MTT assay
    Cytotoxicity against human BGC 823 cells by MTT assay
    [PMID: 18205316]
    Bel-7402 IC50
    5.95 μg/mL
    Compound: 8
    Cytotoxicity against human Bel 7402 cells by MTT assay
    Cytotoxicity against human Bel 7402 cells by MTT assay
    [PMID: 18205316]
    HCT-15 IC50
    48 μM
    Compound: 6
    Cytotoxicity against human HCT-15 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-15 cells incubated for 48 hrs by MTT assay
    [PMID: 33289552]
    HCT-8 IC50
    6.88 μg/mL
    Compound: 8
    Cytotoxicity against human HCT8 cells by MTT assay
    Cytotoxicity against human HCT8 cells by MTT assay
    [PMID: 18205316]
    HeLa IC50
    7 μM
    Compound: 6
    Cytotoxicity against human HeLa cells
    Cytotoxicity against human HeLa cells
    [PMID: 33289552]
    Hep 3B2 IC50
    > 100 μM
    Compound: Compound 4
    Cytotoxicity against human Hep3B cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human Hep3B cells assessed as cell growth inhibition by MTT assay
    [PMID: 27913179]
    LNCaP C4-2B IC50
    4.4 μM
    Compound: 6
    Cytotoxicity against human LNCaP C4-2B cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human LNCaP C4-2B cells incubated for 48 hrs by MTT assay
    [PMID: 33289552]
    MCF7 IC50
    9.1 μM
    Compound: 6
    Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based spectrophotometric assay
    Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based spectrophotometric assay
    [PMID: 33289552]
    MDA-MB-231 IC50
    31 μM
    Compound: 6
    Cytotoxicity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
    [PMID: 33289552]
    RAW264.7 IC50
    0.88 μM
    Compound: 7
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method
    [PMID: 26615888]
    RAW264.7 IC50
    4.9 μM
    Compound: 6
    Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay
    Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay
    [PMID: 26702644]
    UACC-62 IC50
    2.8 μM
    Compound: 6
    Cytotoxicity against human UACC-62 cells incubated for 48 hrs by sulforhodamine B staining based spectrophotometric assay
    Cytotoxicity against human UACC-62 cells incubated for 48 hrs by sulforhodamine B staining based spectrophotometric assay
    [PMID: 33289552]
    In Vitro

    Jolkinolide B (25-100 μg/mL, 24-72 h) reduces viability and induces dose‑ and time‑dependent apoptosis in human leukemic U937 cells. It markedly activates caspase‑3 and caspase‑9, and inhibition of PI3K or XIAP further enhances both apoptosis and caspase activation[1].
    Jolkinolide B (50 μg/mL) induces apoptosis in human leukemic U937 cells and time-dependently modulates apoptosis-related proteins and mRNAs by downregulating phosphorylated Akt, Survivin, XIAP, cIAP1, cIAP2 and upregulating Smac[1].
    Jolkinolide B (1, 5, 10 μM; 24 h) attenuates PA-induced lipotoxicity in mouse primary hepatocytes and Hep3B cells, and 10 μM can restore the Bax/Bcl-2 ratio in primary hepatocytes to normal[3].
    Jolkinolide B (10 μM, 24 h) ameliorates
    Palmitic acid (HY-N0830)-induced mitochondrial dysfunction, lipid accumulation, hepatic steatosis and inflammation in mouse primary hepatocytes and Hep3B cells via inhibiting JAK/STAT3 signaling and regulating downstream lipid synthesis and inflammatory gene expression[3].
    Jolkinolide B (3 μg/mL; 7 days) inhibits the growth of Mycobacterium tuberculosis H37Ra in vitro with an MIC of 3 μg/mL[4].
    Jolkinolide B (3-12 μg/mL; 8 days) inhibits the growth of Mycobacterium tuberculosis H37Ra in 7H9 broth in a concentration- and time-dependent manner over 8 days[4].
    Jolkinolide B (3-6 μg/mL; 2 days) exhibits significant intracellular bactericidal activity against Mycobacterium tuberculosis H37Ra in RAW264.7 macrophages at MOI 5:1 and 10:1[4].
    Jolkinolide B (6 μg/mL; 24 h) alters the morphology of Mycobacterium tuberculosis H37Ra, causing bacilli to become shorter and deformed after 24 hours of treatment[4].
    Jolkinolide B (6 μg/mL; 24 h) alters the transcriptome of Mycobacterium tuberculosis H37Ra after 24 hours of treatment, significantly down-regulating 17 ribosomal protein genes and enriching ribosome-related pathways[4].
    Jolkinolide B (3-6 μg/mL; 24 h) down-regulates the expression of 50S and 30S ribosomal protein genes in Mycobacterium tuberculosis H37Ra[4].
    Jolkinolide B (3-6 μg/mL; 2 days) reduces the number of GFP-expressing Mycobacterium tuberculosis H37Ra in RAW264.7 macrophages[4].

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

    Cell Viability Assay[1]

    Cell Line: human leukemic U937 cells
    Concentration: 25 μg/mL, 50 μg/mL, 100 μg/mL
    Incubation Time: 24 h, 48 h, 72 h
    Result: Reduced U937 cell viability in a dose- and time-dependent manner.
    Decreased viability with increasing drug concentration and exposure time relative to control cells with 98.01% viability.

    Apoptosis Analysis[1]

    Cell Line: human leukemic U937 cells
    Concentration: 25 μg/mL, 50 μg/mL, 100 μg/mL; 50 μg/mL (with 30 min pretreatment of 50 μM LY294002 (HY-10108) or 20 μM Embelin (HY-17473))
    Incubation Time: 48 h (25 μg/mL); 24 h, 48 h, 72 h (50 μg/mL); 48 h (100 μg/mL); 48 h (50 μg/mL with pretreatment)
    Result: Induced apoptosis in U937 cells in a dose- and time-dependent manner.
    Reached ~20% apoptosis rate at 25 μg/mL for 48 h, ~35% at 50 μg/mL for 48 h, ~60% at 100 μg/mL for 48 h.
    Reached ~15% apoptosis rate at 50 μg/mL for 24 h, ~35% at 48 h, ~50% at 72 h.
    Significantly increased the apoptosis rate induced by 50 μg/mL Jolkinolide B for 48 h when cells were pretreated with LY294002 or Embelin.

    Western Blot Analysis[1]

    Cell Line: human leukemic U937 cells
    Concentration: 50 μg/mL
    Incubation Time: 24 h, 48 h, 72 h
    Result: Decreased P-Akt levels in a time-dependent manner, while total Akt levels remained unchanged.
    Decreased the protein expression of Survivin, XIAP, cIAP1, and cIAP2 in a time-dependent manner.
    Increased Smac protein expression in a time-dependent manner.

    Real Time qPCR[1]

    Cell Line: human leukemic U937 cells
    Concentration: 50 μg/mL
    Incubation Time: 24 h, 48 h
    Result: Decreased XIAP and cIAP2 mRNA expression in a time-dependent manner.
    Increased Smac mRNA expression in a time-dependent manner.

    Immunofluorescence[4]

    Cell Line: RAW264.7 macrophages infected with Mycobacterium tuberculosis H37Ra/pCG76-GFP
    Concentration: 3 μg/mL (1×MIC); 6 μg/mL (2×MIC)
    Incubation Time: 2 days
    Result: Reduced the number of GFP-positive M.
    tuberculosis H37Ra/pCG76-GFP bacilli in RAW264.7 macrophages, with a greater reduction observed at 2×MIC compared to 1×MIC.
    In Vivo

    Jolkinolide B (2.5-10 mg/kg; p.o.; daily; 35 days) at 10 mg/kg attenuates allergic airway inflammation and airway remodeling in Ovalbumins (HY-W250978)-induced asthmatic mice by modulating the NF-κB and TGFβ/smad3 pathways[2].

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

    Animal Model: BALB/c (6-week-old male, OVA-induced asthma model)[2]
    Dosage: 2.5 mg/kg; 10 mg/kg
    Administration: p.o.; daily; 35 days
    Result: Reversed OVA-induced allergic airway inflammation and remodeling, restored lung function, and suppressed inflammatory responses and related cytokine secretion.
    Inhibited the activation of NF-κB and TGFβ/smad3 signaling pathways in asthmatic mice.
    Exerted partial effects at 2.5 mg/kg and achieved significant therapeutic efficacy only at 10 mg/kg.
    Molecular Weight

    330.42

    Formula

    C20H26O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@]([C@]1([H])CC2)(CCCC1(C)C)[C@@]([C@@H]3[C@@]4(O5)O3)([H])[C@@]62[C@@H](C4=C(C)C5=O)O6

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 8.33 mg/mL (25.21 mM; ultrasonic and warming and heat to 60°C; 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 3.0265 mL 15.1323 mL 30.2645 mL
    5 mM 0.6053 mL 3.0265 mL 6.0529 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.

    • Molarity Calculator

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.83 mg/mL (2.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  20% HP-β-CD/1% Tween-80 in PBS

      Solubility: 3.33 mg/mL (10.08 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (per animal)

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    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.65%

    References

    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 3.0265 mL 15.1323 mL 30.2645 mL 75.6613 mL
    5 mM 0.6053 mL 3.0265 mL 6.0529 mL 15.1323 mL
    10 mM 0.3026 mL 1.5132 mL 3.0265 mL 7.5661 mL
    15 mM 0.2018 mL 1.0088 mL 2.0176 mL 5.0441 mL
    20 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7831 mL
    25 mM 0.1211 mL 0.6053 mL 1.2106 mL 3.0265 mL
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