Cryptotanshinone

Catalog No.S2285

Cryptotanshinone 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.

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Cryptotanshinone Chemical Structure

Cryptotanshinone Chemical Structure
Molecular Weight: 296.36

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Cryptotanshinone 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.
Targets STAT3 [1]
(HCT-116 cells)
IC50 4.6 μM
LD50
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]
Features

Protocol(Only for 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
Formulation Dissolved in 0.1% solution of sodium lauryl sulfate
Dosages ~600 mg/kg/day
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Shin DS, et al. Cancer Res, 2009, 69(1), 193-202.

[2] Kim EJ, et al. Mol Pharmacol, 2007, 72(1), 62-72.

Chemical Information

Download Cryptotanshinone SDF
Molecular Weight (MW) 296.36
Formula

C19H20O3

CAS No. 35825-57-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 5 mg/mL warming (16.87 mM)
Ethanol 1 mg/mL warming (3.37 mM)
Water <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 2mg/mL
* <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.
Chemical Name Phenanthro[1,2-b]furan-10,11-dione, 1,2,6,7,8,9-hexahydro-1,6,6-trimethyl-, (1R)-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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