2. Epigenetics TGF-beta/Smad Anti-infection Immunology/Inflammation Apoptosis MAPK/ERK Pathway PI3K/Akt/mTOR Cell Cycle/DNA Damage
  3. PKC Influenza Virus NOD-like Receptor (NLR) Apoptosis HBV JNK PI3K Akt CDK Caspase Bcl-2 Family
  4. Daphnoretin

Daphnoretin  (Synonyms: Dephnoretin; Thymelol)

Cat. No.: HY-N0699 Purity: 99.83%
COA
SDS
Handling Instructions Technical Support

Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection.

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

CAS No. : 2034-69-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
20 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Daphnoretin:

Daphnoretin Related Antibodies

Top Publications Citing Use of Products

    Daphnoretin purchased from MedChemExpress. Usage Cited in: J Orthop Surg Res. 2022 Nov 16;17(1):487.  [Abstract]

    Daphnoretin (1, 2, 4 µM) reduces the concentrations of TNF-α, IL-6, and PGE2 in mouse chondrocyte culture supernatant in a dose-dependent manner.

    Daphnoretin purchased from MedChemExpress. Usage Cited in: J Orthop Surg Res. 2022 Nov 16;17(1):487.  [Abstract]

    Daphnoretin or CY-09 markedly attenuates the expression of COX-2, iNOS, TNF-α, IL-6, PGE2 and the NLRP3-ASC-Caspase1 infammasome in ATDC5 cells.

    View All PKC Isoform Specific Products:

    View All Isoforms
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    View All NOD-like Receptor (NLR) Isoform Specific Products:

    View All Isoforms
    NLRP3 NLRP1 NOD1 NOD2

    View All JNK Isoform Specific Products:

    View All Isoforms
    JNK1 JNK2 JNK3 JNK

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    View All Akt Isoform Specific Products:

    View All Isoforms
    Akt Akt1 Akt2 Akt3

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    View All Caspase Isoform Specific Products:

    View All Isoforms
    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

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection[1][2][3][4].

    IC50 & Target[2][3][4]

    PI3K

     

    Akt

     

    NLRP3 inflammasome

     

    Bax

     

    Bcl-2

     

    Caspase-3

     

    Caspase-9

     

    CDK2/cyclinE

     

    JNK

     

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    2 μM
    Compound: Daphnoretin
    Antiproliferative activity human MCF7 cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay
    Antiproliferative activity human MCF7 cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay
    		[PMID: 36154031]
    MDA-MB-231 IC50
    1 μM
    Compound: Daphnoretin
    Antiproliferative activity human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay
    Antiproliferative activity human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay
    		[PMID: 36154031]
    P388 ED50
    2.2 μg/mL
    Compound: Daphnoretin, NSC-291852
    Cytotoxicity against mouse P388 cells
    Cytotoxicity against mouse P388 cells
    		[PMID: 6875580]
    P388 ED50
    3.4 μg/mL
    Compound: daphnoretin
    Cytotoxicity against mouse P388 cells
    Cytotoxicity against mouse P388 cells
    		[PMID: 3783168]
    In Vitro

    Daphnoretin (0.1-1.0 μM; 48 h) inhibits the expression of hepatitis B surface antigen gene at the mRNA level in human hepatocellular carcinoma Hep3B cells, with an IC50 of 0.1 μM after 48 h of treatment[1].
    Daphnoretin (1 μM; 4 h) induces the translocation of protein kinase C (PKC) from the cytosol to the cell membrane, and treatment of human hepatocellular carcinoma Hep3B cells with 800 nM daphnoretin for 24 h downregulates the total intracellular PKC level[1].
    Daphnoretin (0.1-8.0 μM; 24-48 h) inhibits the proliferation of human breast cancer MCF-7 and MDA-MB-231 cells in a concentration- and time-dependent manner, with IC50 values of 2.0 μM and 1.0 μM, respectively[2].
    Daphnoretin (0.5-4 μM; 24 h) induces S-phase cell cycle arrest in human breast cancer MCF-7 and MDA-MB-231 cells by downregulating the protein levels of cyclin E and CDK2[2].
    Daphnoretin (0.5-4 μM; 24 h) induces apoptosis in human breast cancer MCF-7 and MDA-MB-231 cells via a mitochondria-dependent pathway, and reduces BCL-2 levels while increasing the levels of BAX, activated caspase-9 and activated caspase-3[2].
    Daphnoretin (0.5-4 μM; 24 h) inhibits the PI3K/AKT pathway in human breast cancer MCF-7 and MDA-MB-231 cells at 24 h post-treatment by reducing the protein levels of p-PI3K and p-AKT[2].
    Daphnoretin (0.5-512 μM; 48 h) reduces the viability of ATDC5 chondrocytes, with an IC50 of 72.97 μM after 48 h of treatment[3].
    Daphnoretin (1-4 μM; 48 h) increases the viability of IL-1β-induced ATDC5 chondrocytes and reduces their apoptosis rate in a dose-dependent manner[3].
    Daphnoretin (1-4 μM) dose-dependently inhibits IL-1β-induced ERS in ATDC5 chondrocytes[3].
    Daphnoretin (1-4 μM; 48 h) dose-dependently inhibits IL-1β-induced production of inflammatory mediators and activation of the NLRP3 inflammasome in ATDC5 chondrocytes[3].
    Daphnoretin (1.1-30 μM; 6 days) reduces the viability of human CD14+ monocyte-derived dendritic cells in a dose-dependent manner, with an IC50 of approximately 30 μM; at a concentration of 10 μM, it inhibits dendrite formation without significant cytotoxicity[4].
    Daphnoretin (1.1-30 μM; 6 days) dose-dependently downregulates the expression of differentiation and maturation markers, including CD1a, CD40, CD83, DC-SIGN and HLA-DR, on mature dendritic cells derived from human CD14+ monocytes, without inducing their dedifferentiation into macrophages[4].
    Daphnoretin (1.1-30 μM; 6 days) dose-dependently impairs the allostimulatory function of mature dendritic cells derived from human CD14+ monocytes and reduces the proliferative capacity of allogeneic naive CD4+CD45RA+ T cells[4].
    Daphnoretin (10 μM) specifically downregulates the LPS-induced upregulated expression of phosphorylated JNK in human CD14+ monocyte-derived dendritic cells[4].

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

    Daphnoretin Related Antibodies

    Western Blot Analysis[1]

    Cell Line: human hepatoma Hep3B cells
    Concentration: 1 μM (PKC translocation); 800 nM (PKC down-regulation)
    Incubation Time: 4 h (PKC translocation); 24 h (PKC down-regulation)
    Result: Increased membrane-bound PKC by ~20-fold with a concomitant decrease in cytosolic PKC after 4 h of 1 μM treatment. Diminished total extractable cellular PKC to a barely detectable level after 24 h of 800 nM treatment.

    Cell Cycle Analysis[2]

    Cell Line: human breast cancer MCF-7, human breast cancer MDA-MB-231
    Concentration: 1, 2, and 4 μM (MCF-7); 0.5, 1 and 2 μM (MDA-MB-231)
    Incubation Time: 24 h (cell cycle assay; Western blot)
    Result: Significantly increased the proportion of MCF-7 and MDA-MB-231 cells arrested in the S phase.
    Significantly downregulated the protein levels of cyclin E and CDK2 in both cell lines compared to controls.

    Apoptosis Analysis[2]

    Cell Line: human breast cancer MCF-7, human breast cancer MDA-MB-231
    Concentration: 1, 2, and 4 μM (MCF-7); 0.5, 1 and 2 μM (MDA-MB-231)
    Incubation Time: 24 h (apoptosis assays; Western blot)
    Result: Revealed typical apoptotic features (chromatin/nuclear condensation, apoptotic bodies) in both daphnoretin-treated cell lines via Hoechst 33258 staining.
    Showed significantly increased apoptotic rates in treated MCF-7 and MDA-MB-231 cells compared to controls.
    Significantly downregulated BCL-2 protein levels and upregulated BAX, cleaved caspase-9, and cleaved caspase-3 protein levels in both cell lines.

    Western Blot Analysis[2]

    Cell Line: human breast cancer MCF-7, human breast cancer MDA-MB-231
    Concentration: 1, 2 and 4 μM (MCF-7, 24 h); 0.5-2 μM (MDA-MB-231, 24 h); 0.5, 1 and 2 μM (0.5, 1, 2 h, both cell lines)
    Incubation Time: 24 h (24 h treatment group); 0.5 h, 1 h, 2 h (short-term treatment group)
    Result: Significantly downregulated the protein levels of p-PI3K and p-AKT in both MCF-7 and MDA-MB-231 cells after 24 h of treatment.
    Showed no significant changes in p-PI3K or p-AKT levels after 0.5, 1, or 2 h of treatment in either cell line.
    Caused no significant alterations in total PI3K and AKT levels.
    In Vivo

    Daphnoretin (10 mg/kg; i.p.; administered daily for the first week post-surgery, then once every 3 days for the subsequent 7 weeks; total duration of 8 weeks) alleviates the progression of osteoarthritis induced by destabilization of the medial meniscus (DMM) in mice by attenuating cartilage damage, regulating the expression of apoptosis-related proteins, inhibiting endoplasmic reticulum stress and inactivating the NLRP3 inflammasome, significantly reducing the OARSI score and improving the thickness of the subchondral cortical bone plate[3].
    Daphnoretin (0.5-1.0 mg/kg; i.p.; once daily for 7 days) inhibits acute skin allograft rejection in mice without altering body weight or white blood cell counts, and exhibits no obvious dose-dependent effect[4].

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

    Animal Model: C57BL/6 (8-10-week-old male, DMM-induced OA)[3]
    Dosage: 10 mg/kg
    Administration: i.p.; daily (first week post-surgery), once every 3 days (subsequent 7 weeks); 8 weeks total
    Result: Repaired the articular cartilage surface relative to the OA-only group.
    Increased the thickness of cartilage and subchondral cortical bone plate relative to the OA-only group.
    Reduced the number of TRAP-positive cells relative to the OA-only group.
    Significantly improved the thickness of the subchondral cortical bone plate relative to the OA-only group.
    Reduced the OARSI score relative to the OA-only group.Downregulated the expression of pro-apoptotic proteins Bax and cleaved-caspase3 in cartilage tissue relative to the OA-only group.
    Upregulated the anti-apoptotic protein Bcl2 in cartilage tissue relative to the OA-only group.
    Reduced the expression of endoplasmic reticulum stress markers GRP78, CHOP, ATF6, and Caspase-12 relative to the OA-only group.
    Reduced the expression of NLRP3, ASC, and Caspase-1 components of the NLRP3 inflammasome relative to the OA-only group.
    Abated the mRNA levels of Cox-2, inos, Tnf-α, and Il-6 in cartilage tissues relative to the OA-only group.
    Animal Model: C57BL/6 (H-2b) (male, 6-8-week-old); BALB/c (H-2d) (male, 6-8-week-old, skin allograft recipient)[4]
    Dosage: 0.5 mg/kg; 1.0 mg/kg
    Administration: i.p.; once daily for 7 days
    Result: Increased the survival fraction of skin allografts relative to untreated controls.
    Caused no significant changes in recipient body weight or white blood cell count during the observation period.
    Showed no evident dose-dependent response between the two tested doses.
    Molecular Weight

    352.29

    Formula

    C19H12O7
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C1C(OC2=CC=C(C(O3)=C2)C=CC3=O)=CC4=CC(OC)=C(O)C=C4O1
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (70.96 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 2.8386 mL 14.1929 mL 28.3857 mL
    5 mM 0.5677 mL 2.8386 mL 5.6771 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

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (5.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (5.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.83%

    SDS (393 KB)

    COA (246 KB)

    Handling Instructions (2659 KB)
    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 2.8386 mL 14.1929 mL 28.3857 mL 70.9643 mL
    5 mM 0.5677 mL 2.8386 mL 5.6771 mL 14.1929 mL
    10 mM 0.2839 mL 1.4193 mL 2.8386 mL 7.0964 mL
    15 mM 0.1892 mL 0.9462 mL 1.8924 mL 4.7310 mL
    20 mM 0.1419 mL 0.7096 mL 1.4193 mL 3.5482 mL
    25 mM 0.1135 mL 0.5677 mL 1.1354 mL 2.8386 mL
    30 mM 0.0946 mL 0.4731 mL 0.9462 mL 2.3655 mL
    40 mM 0.0710 mL 0.3548 mL 0.7096 mL 1.7741 mL
    50 mM 0.0568 mL 0.2839 mL 0.5677 mL 1.4193 mL
    60 mM 0.0473 mL 0.2365 mL 0.4731 mL 1.1827 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Daphnoretin Related Classifications

    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.

    Keywords:

    Daphnoretin2034-69-7Dephnoretin ThymelolPKCInfluenza VirusNOD-like Receptor (NLR)ApoptosisHBVJNKPI3KAktCDKCaspaseBcl-2 FamilyProtein kinase CHepatitis B virusc-Jun N-terminal kinasePhosphoinositide 3-kinasePKBProtein kinase BCyclin dependent kinaseCD14? monocyte-derived dendritic cellsPI3K/AKT pathwayMCF-7 cellsATDC5 chondrocyteshepatitis B surface antigenNLRP3 inflammasomeProtein Kinase CHep3B cellsMDA-MB-231 cellsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Daphnoretin
    Cat. No.:
    HY-N0699
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.