1. JAK/STAT Signaling Stem Cell/Wnt Autophagy
  2. STAT Autophagy
  3. Cryptotanshinone

Cryptotanshinone  (Synonyms: Cryptotanshinon; Tanshinone c)

Cat. No.: HY-N0174 Purity: 98.70%
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Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.

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

Cryptotanshinone Chemical Structure

Cryptotanshinone Chemical Structure

CAS No. : 35825-57-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 197 In-stock
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Cryptotanshinone:

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Cryptotanshinone

IF
WB

    Cryptotanshinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2022 Nov 30;175434.  [Abstract]

    Cryptotanshinone (CTS; 10, 20 μМ; 24 h) promotes apoptosis of BPH-1 (fig A) and WPMY-1 (fig B) cells.

    Cryptotanshinone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2022 Nov 30;175434.  [Abstract]

    Cryptotanshinone (CTS; 0, 10, 20 μМ; 24 h) significantly decreases the expression of Col-I and (when at 20 μМ) Col-III, α-SMA, in WPMY-1 cells.

    View All STAT Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.

    IC50 & Target[1]

    STAT3

    4.6 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    AGS IC50
    1.58 μM
    Compound: 3, cryptotanshinone
    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
    10.2 μM
    Compound: 3, cryptotanshinone
    Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay
    Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    AGS IC50
    13.5 μM
    Compound: 3, cryptotanshinone
    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]
    BaF3 IC50
    17.22 μM
    Compound: Cryptotanshinone
    Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay
    Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay
    [PMID: 23957426]
    ECa-109 cell line IC50
    5.01 μM
    Compound: 8
    Antitumor activity against human EC109 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antitumor activity against human EC109 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 35504209]
    HCT-116 IC50
    4.6 μM
    Compound: 47
    Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay
    Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22650325]
    Hep 3B2 IC50
    > 30 μM
    Compound: 3, cryptotanshinone
    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]
    Hep 3B2 IC50
    > 30 μM
    Compound: 3, cryptotanshinone
    Viability of human Hep3B cells under hypoxic conditions after 24 hrs by MTT assay
    Viability of human Hep3B cells under hypoxic conditions after 24 hrs by MTT assay
    [PMID: 17583950]
    Hep 3B2 IC50
    1.36 μM
    Compound: 3, cryptotanshinone
    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]
    HepG2 IC50
    29.2 μM
    Compound: 8
    Antitumor activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antitumor activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 35504209]
    KB 3-1 IC50
    6.9 μM
    Compound: 1
    Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay
    Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay
    [PMID: 11720520]
    KB-V1 IC50
    7.5 μM
    Compound: 1
    Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay
    Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay
    [PMID: 11720520]
    MIA PaCa-2 IC50
    5.8 μM
    Compound: 14
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
    [PMID: 21775156]
    Vero C1008 CC50
    > 300 μM
    Compound: 28
    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

    Cryptotanshinone significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705 phosphorylation and the dimerization of STAT3, compared to tanshinone IIA which exhibits no activity. Cryptotanshinone (7 μM) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of appr 5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR, suggesting the inhibition of STAT3 Tyr705 phosphorylation might due to a direct mechanism probably by binding to the SH2 domain of STAT3. Cryptotanshinone significantly inhibits the proliferation of DU145 prostate cancer cells harboring constitutively active STAT3 with GI50 of 7 μM by blocking STAT3 activity, which leads to the down-regulation of cyclin D1, Bcl-xL, and survivin, subsequently the accumulation in the G0-G1 phase. Cryptotanshinone exhibits less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells[1]. Cryptotanshinone significantly attenuates the in vitro hormonal effects of DEX on ovaries, as indicated by a significant decrease in T and an increase in P levels in the culture medium. Cryptotanshinone significantly increases the levels of phosphorylated AKT2 and GSK3β in the DEX-treated ovaries[2]. Cotreatment with imatinib and Cryptotanshinone shows a significant synergistic killing effect in both imatinib sensitive and resistant CML cell lines, as well as primary CML cells[3].

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

    In Vivo

    Cryptotanshinone reverses the ovarian IR and significantly increases 2-deoxy-D-[1,2-3H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rate and plasma E2 and P levels[2]. Cryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period[4].

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

    Molecular Weight

    296.36

    Formula

    C19H20O3

    CAS No.
    Appearance

    Solid

    Color

    Pink to red

    SMILES

    O=C(C1=C2C=CC3=C1CCCC3(C)C)C(C4=C2OC[C@@H]4C)=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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (16.87 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)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3743 mL 16.8714 mL 33.7427 mL
    5 mM 0.6749 mL 3.3743 mL 6.7485 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 0.83 mg/mL (2.80 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 0.83 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 (8.3 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: ≥ 0.83 mg/mL (2.80 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.

    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:  Corn Oil

      Solubility: 8 mg/mL (26.99 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (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:
    %
    DMSO +
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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).
    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: 98.70%

    References
    Kinase Assay
    [1]

    HCT-116 cells are transiently transfected with reporter plasmid having the STAT3-binding element for regulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of 0.2 to 50 μM. After treatment, cells are harvested in 20 μL of passive lysis buffer and luciferase activity is evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of Cryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.

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

    Cell Assay
    [3]

    The MTT assay is used for the assessment of cell growth inhibition as described previously. Cells are seeded at a density of 8000 cells per well in 96-well plates in RPMI-1640 containing 10% FBS. Different concentrations of imatinib and CPT are added and incubated for another 24 h. Then, 20 μL of MTT are added into each well and the absorbance at 570 nm is measured on an enzyme linked immunosorbent assay (ELISA) plate reader. The coefficient of drug interaction (CDI) between imatinib and CPT is determined according to a previous study. The calculated method is as follows: CDI/AB/(A × B). According to the absorbance of each group, AB is the ratio of the combination group to the control group; A or B is the ratio of the single agent group to the control group. CDI < 1 indicates a synergistic effect; CDI=1 indicates an additive effect; CDI > 1 indicates an antagonistic effect. In the combination treatment group, the concentrations of CPT are arbitrarily designated according to the 50% inhibitory concentration (IC50) value. Then, the cell viabilities are determined after treatment with different concentrations of imatinib plus CPT (constant CPT concentration for one cell type). Finally, the combination IC50 values of imatinib are calculated, and are represented in Table I. The primary CML cells CP1 to CP3 are isolated from patients in chronic phase, while BC1 and BC2 are isolated from patients in blast crisis. Three independent sets of experiments are performed. The IC50 values are presented as the mean±standard deviation (SD).

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3743 mL 16.8714 mL 33.7427 mL 84.3569 mL
    5 mM 0.6749 mL 3.3743 mL 6.7485 mL 16.8714 mL
    10 mM 0.3374 mL 1.6871 mL 3.3743 mL 8.4357 mL
    15 mM 0.2250 mL 1.1248 mL 2.2495 mL 5.6238 mL
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      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.

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    Product Name:
    Cryptotanshinone
    Cat. No.:
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