Name: Cryptotanshinone (Tanshinone C)
Brand: Selleck Chemicals
SKU: S2285
Availability: InStock
Rating: 5 (71 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	EGFR JAK Pim
Other STAT Inhibitors	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) SH-4-54 C188-9 (TTI-101) BP-1-102 HO-3867 Nifuroxazide AS1517499 Homoharringtonine (HHT)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Solubility

In vitro
Batch:

Ethanol : 10 mg/mL

DMSO : 8 mg/mL (26.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (4.22mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	296.36	Formula	C₁₉H₂₀O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	35825-57-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	STAT3 (HCT-116 cells) 4.6 μM
In vitro	Cryptotanshinone (Tanshinone C), 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. At 7 μM, it 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. This compound 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. It exhibits less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells.
Kinase Assay	STAT3-dependent dual-luciferase assay
Kinase Assay	HCT-116 cells are transiently transfected with a reporter plasmid containing the STAT3-binding element for regulating luciferase assay. These cells are treated with Cryptotanshinone (Tanshinone C) 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 using the Dual Luciferase Reporter Assay kit on a Wallac Victor2. The concentration of this compound that inhibits luciferase activity by 50% represents the IC50 value.
In vivo	Cryptotanshinone (Tanshinone C) administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lep^ob) and diet-induced obese (DIO) mice in a dose-dependent manner. It 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 this compound at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lep^ob), db/db mice (C57BL/KsJ-Lepr^db), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19118003/ [2] https://pubmed.ncbi.nlm.nih.gov/17429005/

Applications

Methods	Biomarkers	PMID
Western blot	p-STAT3 / STAT3 / p-ERK / ERK	30986607
Immunofluorescence	p-STAT3 / p-ERK	30986607
Growth inhibition assay	Cell viability	20820782

Tech Support

Handling Instructions

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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:
It 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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Cryptotanshinone (Tanshinone C) STAT inhibitor

Chemical Structure

Molecular Weight: 296.36