Cryptotanshinone (Tanshinone C)

Catalog No.S2285 Batch:S228504

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Technical Data

Formula

C19H20O3
Molecular Weight 296.36 CAS No. 35825-57-1
Solubility (25°C)* In vitro DMSO 8 mg/mL (26.99 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Targets
STAT3 [1]
(HCT-116 cells)
4.6 μM
In vitro Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), 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 ~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]
In vivo 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. [2]

Protocol (from reference)

Kinase Assay:[1]
  • STAT3-dependent dual-luciferase assay

    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.
Cell Assay:[1]
  • Cell lines

    KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116

  • Concentrations

    Dissolved in DMSO, final concentrations ~50 μM

  • Incubation Time

    24 or 48 hours

  • Method

    Cells are exposed to Cryptotanshinone for 24 or 48 hours. For the determination of cell proliferation, the cell proliferation reagent WST-1 is added and WST-1 formazan is quantitatively measured at 450 nm using an ELISA reader.
Animal Study:[2]
  • Animal Models

    Zucker Diabetic Fatty (ZDF) (male) type 2 diabetic rat, ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb) and male C57BL/6J mice with high-fat diet-induced obesity

  • Dosages

    ~600 mg/kg/day

  • Administration

    Orally

Customer Product Validation

Data from [Data independently produced by , , Nat Commun, 2017, 8:14290]

Data from [Data independently produced by , , Diabetes, 2018, 67(2):235-247]

Data from [Data independently produced by , , Cancer Lett, 2018, 416:24-30]

Data from [Data independently produced by , , EBioMedicine, 2018, 36:358-366]

Selleck's Cryptotanshinone (Tanshinone C) has been cited by 70 publications

PEDF peptide plus hyaluronic acid stimulates cartilage regeneration in osteoarthritis via STAT3-mediated chondrogenesis [ Bone Joint Res, 2024, 13(4):137-148] PubMed: 38555936
Revisiting the role of endogenous STAT3 in HPV-positive cervical cancer cells [ J Med Virol, 2023, 95(11):e29230] PubMed: 38009614
Galectin-9 Facilitates Epstein-Barr Virus Latent Infection and Lymphomagenesis in Human B Cells [ Microbiol Spectr, 2023, e0493222.] PubMed: 36622166
Inhibitory Effect and Mechanism of Ursolic Acid on Cisplatin-Induced Resistance and Stemness in Human Lung Cancer A549 Cells [ Evid Based Complement Alternat Med, 2023, 2023:1307323] PubMed: 37089712
Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632] PubMed: 37828768
Bile Acid-Microbiome Interaction Promotes Gastric Carcinogenesis [ Adv Sci (Weinh), 2022, e2200263] PubMed: 35285172
B7-H4 expression is upregulated by PKCδ activation and contributes to PKCδ-induced cell motility in colorectal cancer [ Cancer Cell Int, 2022, 22(1):147] PubMed: 35410218
The endosomal pH regulator NHE9 is a driver of stemness in glioblastoma [ PNAS Nexus, 2022, 1(1):pgac013] PubMed: 35387234
USP24-GSDMB complex promotes bladder cancer proliferation via activation of the STAT3 pathway [ Int J Biol Sci, 2021, 17(10):2417-2429] PubMed: N/A
The Antimicrobial Peptide Human β-Defensin-3 Accelerates Wound Healing by Promoting Angiogenesis, Cell Migration, and Proliferation Through the FGFR/JAK2/STAT3 Signaling Pathway [ Front Immunol, 2021, 12:712781] PubMed: 34594328

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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