Home JAK/STAT STAT inhibitor - Apoptosis related activator - Autophagy activator Cryptotanshinone (Tanshinone C) For research use only.

Cryptotanshinone (Tanshinone C)

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.

Cryptotanshinone (Tanshinone C) Chemical Structure

Cryptotanshinone (Tanshinone C) Chemical Structure

CAS No. 35825-57-1

Purity & Quality Control

Cryptotanshinone (Tanshinone C) Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-3-1 Cytotoxicity assay 48 hrs Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay, IC50=6.9μM 11720520
KBV1 Cytotoxicity assay 48 hrs Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay, IC50=7.5μM 11720520
OVCAR-3 Cytotoxicity assay Cytotoxicity against human OVCAR-3 cells by MTT assay, CD50=9.12μM 16038550
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells by MTT assay, CD50=17.2μM 16038550
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells by MTT assay, CD50=29.7μM 16038550
Hep3B Function assay 16 hrs Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay, IC50=1.36μM 17583950
AGS Function assay 16 hrs Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay, IC50=1.58μM 17583950
AGS Function assay 24 hrs Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay, IC50=10.2μM 17583950
AGS Function assay 24 hrs Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay, IC50=13.5μM 17583950
THLE3 Cytotoxicity assay Cytotoxicity against human THLE3 cells by MTT assay, EC50=22.9μM 20455578
HepG2 Apoptosis assay Induction of apoptosis in human HepG2 cells expressing wild type p53 gene assessed as caspase 3 activation 20455578
MIAPaCa2 Cytotoxicity assay 24 hrs Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay, IC50=5.8μM 21775156
HCT116 Function assay 24 hrs Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay, IC50=4.6μM 22650325
BA/F3 Growth inhibition assay 48 hrs Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay, IC50=17.22μM 23957426
U-973 Cell cycle assay 15 to 30 uM 24 hrs Cell cycle arrest at G1-S phase in PTPN11 G60R mutant harboring human U-973 cells at 15 to 30 uM after 24 hrs by FACS analysis 23957426
U-973 Apoptosis assay 15 to 30 uM 24 hrs Induction of apoptosis in PTPN11 G60R mutant harboring human U-973 cells at 15 to 30 uM after 24 hrs by FACS analysis 23957426
PTPN11 Function assay 1.5 to 6 uM 14 days Inhibition of GM-CSF-induced growth in PTPN11 E76K/+ myeloid progenitor cells from JMML patient at 1.5 to 6 uM after 14 days by inverted microscopic analysis 23957426
PTPN11 Function assay 1.5 to 6 uM 14 days Inhibition of GM-CSF-induced colony formation in PTPN11 E76K/+ myeloid progenitor cells from JMML patient at 1.5 to 6 uM after 14 days by inverted microscopic analysis 23957426
PTPN11 Function assay 1.5 to 15 uM 7 days Inhibition of GM-CSF-induced colony formation in PTPN11 E76K/+/Mxl-Cre+ mouse myeloid progenitor cells at 1.5 to 15 uM after 7 days by inverted microscopic analysis 23957426
HeLa Growth inhibition assay 24 hrs Growth inhibition of human HeLa cells after 24 hrs 23957426
Ba/F3 Function assay 30 uM 3 hrs Inhibition of IL3-induced SHP2-Gab2 interaction in mouse Ba/F3 cells pretreated at 30 uM for 3 hrs prior IL3 stimulation by immunoblotting method 23957426
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / p-ERK / ERK 30986607
Immunofluorescence p-STAT3 / p-ERK 30986607
Growth inhibition assay Cell viability 20820782
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 296.36 Formula

C19H20O3
CAS No. 35825-57-1 SDF Download Cryptotanshinone (Tanshinone C) SDF
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 10 mg/mL

DMSO : 8 mg/mL ( (26.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
I want to use this compound for my mouse in vivo experiment, so how to reconstitute it?

Answer:
Cryptotanshinone can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 2 mg/ml. But after stayed for about 0.5-1 hour, the precipitation went out. So if you are going to use this vehicle, it is recommended to be prepared just before use.

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