2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. Tanshinone I

Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).

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

CAS No. : 568-73-0

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Tanshinone I:

Tanshinone I Related Antibodies

Top Publications Citing Use of Products

    Tanshinone I purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 3;23(19):11721.

    PANC-1 and AsPC-1 cells were treated with various concentrations (0.5–5 µM) of Tanshinone I for various time periods, as indicated. Cell proliferation was analyzed by MTT assay.

    Tanshinone I purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 3;23(19):11721.

    PANC-1 and AsPC-1 cells were incubated with 5 µM Tanshinone I for 72 h; lipid peroxidation was analyzed by flow cytometry.

    Tanshinone I purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 3;23(19):11721.

    PANC-1 cells were incubated with Tanshinone I (5–10 µM) for 72 h. The mRNA levels of fatty acid synthesis-related genes were quantified by qRT-PCR.

    Tanshinone I purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 3;23(19):11721.

    AsPC-1 cells were incubated with Tanshinone I (1–10 µM) for 72 h. FASN protein level was analyzed by western blot analysis.

    Tanshinone I purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Oct 3;23(19):11721.

    PANC-1 and AsPC-1 cells were treated with 5 µM Tanshinone I and incubated for two weeks to form colonies.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).

    IC50 & Target

    IC50: 11 μM (sPLA2), 82 μM (cPLA2)[1].
    Cellular Effect
    Cell Line Type Value Description References
    AGS IC50
    12.5 μM
    Compound: 6, tanshinone i
    Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    		[PMID: 17583950]
    AGS IC50
    > 50 μM
    Compound: 6, tanshinone i
    Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay
    Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay
    		[PMID: 17583950]
    Hep 3B2 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human Hep3B cells deficient in p53 gene by MTT assay
    Cytotoxicity against human Hep3B cells deficient in p53 gene by MTT assay
    		[PMID: 20455578]
    Hep 3B2 IC50
    8.51 μM
    Compound: 6, tanshinone i
    Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
    		[PMID: 17583950]
    Hep 3B2 IC50
    > 50 μM
    Compound: 6, tanshinone i
    Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay
    Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay
    		[PMID: 17583950]
    HepG2 EC50
    6.3 μM
    Compound: 3
    Cytotoxicity against human HepG2 cells expressing wild type p53 gene by MTT assay
    Cytotoxicity against human HepG2 cells expressing wild type p53 gene by MTT assay
    		[PMID: 20455578]
    HepG2 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against doxorubicin resistant human HepG2 cells expressing wild type p53 gene by MTT assay
    Cytotoxicity against doxorubicin resistant human HepG2 cells expressing wild type p53 gene by MTT assay
    		[PMID: 20455578]
    KB IC50
    5.87 μM
    Compound: 1
    Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay
    		[PMID: 29294282]
    MCF7 ED50
    0.82 μg/mL
    Compound: Tanshinone I
    Dose required for reduction in cell growth of human breast cancer MCF-7 cell line
    Dose required for reduction in cell growth of human breast cancer MCF-7 cell line
    		[PMID: 15509181]
    MCF7 IC50
    7.927 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 33751939]
    MDA-MB-231 ED50
    0.75 μg/mL
    Compound: Tanshinone I
    Dose required for reduction in cell growth of human breast cancer MDA-MB-231 cell line
    Dose required for reduction in cell growth of human breast cancer MDA-MB-231 cell line
    		[PMID: 15509181]
    MDA-MB-231 IC50
    7.962 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 33751939]
    MIA PaCa-2 IC50
    10.5 μM
    Compound: 15
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    		[PMID: 21775156]
    PLC-PRF-5 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human PLC/PRF/5 cells expressing mutant p53 gene (codon 249) by MTT assay
    Cytotoxicity against human PLC/PRF/5 cells expressing mutant p53 gene (codon 249) by MTT assay
    		[PMID: 20455578]
    Vero C1008 CC50
    > 200 μM
    Compound: 29
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    		[PMID: 35620927]
    In Vitro

    Tanshinone I inhibits PGE2 formation from LPS-induced RAW macrophages (IC50=38 μM). When Tanshinone I is added simultaneously with LPS, this compound clearly inhibits PGE2 production (IC50=38 μM) at 10-100 μM. Tanshinone I also reduces PGE2 production (IC50=46 μM) when added after COX-2 is fully induced. The fact that Tanshinone I inhibits PGE2 production by pre-induced COX-2 strongly suggests that this compound may directly inhibit COX-2 activity and/or affect PLA2 activity. When Tanshinone I is incubated with two different forms of phospholipase A2 (PLA2), it clearly inhibits sPLA2 (IC50=11 μM) in a concentration-dependent manner. Although being less potent, Tanshinone I also inhibits cPLA2 (IC50=82 μM)[1].

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

    Tanshinone I Related Antibodies
    In Vivo

    Tanshinone I shows antiinflammatory activity in rat carrageenan-induced paw oedema and adjuvant-induced arthritis. In order to establish the anti-inflammatory activity of Tanshinone I, the classical animal models of acute and chronic inflammation [rat carrageenan (CGN)-induced paw oedema and rat adjuvant-induced arthritis (AIA)] are employed. When Tanshinone I is orally administered, it shows significant anti-inflammatory activity against CGN-induced paw oedema (47% inhibition at 160 mg/kg), while the IC50 of indomethacin is 7.1 mg/kg. In AIA, Tanshinone I gives 27% inhibition of secondary inflammation at 18 day with an oral dose of 50 mg/kg/day, whereas prednisolone (5 mg/kg/day) shows potent inhibition (65%)[1].

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

    276.29

    Formula

    C18H12O3
    CAS No.
    Appearance

    Solid

    Color

    Light brown to black

    SMILES

    O=C(C1=C2C=CC3=C1C=CC=C3C)C(C4=C2OC=C4C)=O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 2 mg/mL (7.24 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 3.6194 mL 18.0969 mL 36.1939 mL
    5 mM 0.7239 mL 3.6194 mL 7.2388 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 98.83%

    SDS (396 KB)

    COA (257 KB) HNMR (365 KB) RP-HPLC (247 KB) MS (73 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    As sources of PLA2, human recombinant sPLA2 (type IIA) is purified from CHO cells transfected with the PLA2 gene and rabbit recombinant platelet cPLA2 is obtained through its expression in baculovirus. The standard reaction mixture (200 μL) contained 100 mM Tris-HCl buffer (pH 9.0) with 6 mM CaCl2 and 20 nmol 1-acyl-[1-14C]-arachidonyl-sn-glycerophosphoethanolamine (2000 cpm/nmol) in the presence or absence of Tanshinone I. The reaction is started by adding 50 ng purified sPLA2 or cPLA2. After 20 min at 37°C, the free fatty acid generated is analysed. Under these standard conditions, the reaction mixture in the absence of Tanshinone I released approximately 10% of free fatty acid from the phospholipid substrate added[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    RAW 264.7 cells are cultured with DMEM supplemented with 10% FBS and 1% antibiotics under 5% CO2 at 37°C. Briefly, cells are plated in 96-well plates (2×105 cells/well). LPS (1 ug/mL) and Tanshinone I are simultaneously added and incubated for 24 h, unless otherwise specified. The PGE2 concentration in the medium is measured using an EIA kit for PGE2. In order to determine the effects of Tanshinone I on PGE2 production after induction of COX-2, cells are incubated with LPS (1 ug/mL) for 24 h and thoroughly washed. Then, Tanshinone I is added without LPS and the cells are incubated for another 24 h. From the medium, PGE2 concentrations are measured. The cytotoxicity of Tanshinone I to RAW cells is checked using the MTT assay. Tanshinone I does not show any cytotoxicity up to 100 uM[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    In order to evaluate the inhibitory activity of Tanshinone I against animal models of acute and chronic inflammation, rat carrageenan (CGN)-induced paw oedema and adjuvant-induced arthritis (AIA) models are employed. Briefly, 1% CGN dissolved in pyrogen-free saline (0.05 mL) is injected into right hind paw of rats for the paw oedema test. After 5 h, swelling of the treated paw is measured using a plethysmometer. Tanshinone I dissolved in 0.5% CMC is administered orally 1 h prior to CGN injection. For the AIA test, an arthritic inflammation is provoked by injection of Mycobacterium Butyricum (0.6 mL/rat) dissolved in mineral oil to the right hind paw of rats. Tanshinone I is orally administered every day. The swelling of the treated and untreated paws is measured using a plethysmometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6194 mL 18.0969 mL 36.1939 mL 90.4846 mL
    5 mM 0.7239 mL 3.6194 mL 7.2388 mL 18.0969 mL
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    Tanshinone I 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:

    Tanshinone I568-73-0Tanshinone APhospholipaseInhibitorinhibitorinhibit

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