Cryptotanshinone

Catalog No.S2285

Cryptotanshinone Chemical Structure

Molecular Weight(MW): 296.36

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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Cited by 22 Publications

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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)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Hep3B cells NHXYZoVHfW6ldHnvckBie3OjeR?= MoryNVYhcA>? MnfCTY5pcWKrdHnvckBw\iCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhdHWlaX\ldoF{\SCneIDy[ZN{cW:wIHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2xMlM3KM7:TR?= MYOxO|U5Ozl3MB?=
human AGS cells M1[zVGZ2dmO2aX;uJIF{e2G7 MmXBNVYhcA>? MVrJcohq[mm2aX;uJI9nKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBCT1NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgXCxeHnhMYlv\HWlZXSgcJVkcW[ncnHz[UBmgHC{ZYPzbY9vKGGodHXyJFE3KGi{czDifUBz\XCxcoTldkBie3OjeTygTWM2OD1zLkW4JO69VQ>? M{G1N|E4PTh|OUWw
human HCT116 cells M4ja[GZ2dmO2aX;uJIF{e2G7 M{niSVI1KGh? MYnJcohq[mm2aX;uJI9nKFOWQWSzJIV5eHKnc4Pl[EBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygbYM2OD12Lk[g{txO Ml3iNlI3PTB|MkW=
human MIAPaCa2 cells NWfLRnBGS3m2b4TvfIlkyqCjc4PhfS=> M1PXRVI1KGh? NVm4bmE6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13Lkig{txO NXrtNnI6OjF5N{WxOVY>
human KB-3-1 cells NWjjcFlMS3m2b4TvfIlkyqCjc4PhfS=> MoLMOFghcA>? NWjRWJV[S3m2b4TvfIlkcXS7IHHnZYlve3RiZIL1[{1{\W6|aYTpeoUhcHWvYX6gT2IuOy1zIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFNxUF3TJIF{e2G7LDDJR|UxRTZwOTFOwG0> MnHINVE4OjB3MkC=
human KBV1 cells MmrQR5l1d3SxeHnjxsBie3OjeR?= NWfwO5FuPDhiaB?= NIfjWJBEgXSxdH;4bYNqfHliYXfhbY5{fCCvdXz0bYRzfWdvcnXzbZN1[W62IHj1cYFvKEuEVkGgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WUz;QUXMh[XO|YYmsJGlEPTB;Nz61JO69VQ>? MVixNVczODV{MB?=
human AGS cells MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWKyOEBp NWP1ZZltXmmjYnnsbZR6KG:oIHj1cYFvKEGJUzDj[YxteyC3bnTldkBpgXCxeHnjJINwdmSrdHnvcpMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNE4zKM7:TR?= NHP2RosyPzV6M{m1NC=>
human THLE3 cells M{OwN2N6fG:2b4jpZ:Kh[XO|YYm= NWXlbVFvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiORUOgZ4VtdHNiYomgUXRVKGG|c3H5MEBGSzVyPUKyMlkh|ryP Mo\lNlA1PTV3N{i=
human PBMC MYDGeY5kfGmxbjDhd5NigQ>? NYXNSXZoUW6qaXLpeIlwdiCxZjDwbJl1d2inbXHn[4x2fGmwaX7pckBCNXO2aX31cIF1\WRiaIXtZY4hWEKPQzDwdo9tcW[ncnH0bY9vKGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJHsyPEOfdHj5cYllcW6nIHnuZ49zeG:{YYTpc44tKEmFNUC9N|cvPCEQvF2= NV3Nbo9zOTF5MkC1NlA>
PTPN11 E76K/+ MEF M1\qZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVSyNEDPxE1? NUDhW2JvT3Kxd4ToJIlvcGmkaYTpc44hd2ZiUGTQUlEyKEV5NluvL{BOTUZiYYSgNlAhfU1? M3zpc|I{QTV5NEK2
human HeLa cells NWfNfZBDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUeyOEBp M2ToS2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgNlQhcHK| MoLyNlM6PTd2Mk[=
human HepG2 cells NV;QbWw5S3m2b4TvfIlkyqCjc4PhfS=> M3HmXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGK7IF3UWEBie3OjeR?= MUCxOlA{QDV3MB?=
human OVCAR-3 cells M2j1W2N6fG:2b4jpZ:Kh[XO|YYm= NH7B[VFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUj2zJINmdGy|IHL5JG1VXCCjc4PhfS=> NYTxb5dTOTZyM{i1OVA>
mouse Ba/F3 cells MYnGeY5kfGmxbjDhd5NigQ>? MnPON|Ah|ryP M4jyWlMhcA>? NXPwbWJnUW6qaXLpeIlwdiCxZjDJUFMucW6mdXPl[EBUUFB{LVfhZlIhcW62ZYLhZ5Rqd25iaX6gcY92e2ViQnGvSlMh[2WubIOgdJJmfHKnYYTl[EBifCB|MDD1UUBnd3JiMzDodpMheHKrb4KgTWw{KHO2aX31cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6pIH3leIhw\A>? NHv6[W4zOzl3N{SyOi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-ERK / ERK ; 

PubMed: 30986607     


Immunoblotting of pSTAT3 (Y705) and pERK1/2 in U251/C7 cells treated with cryptotanshinone (10 μM) for 0, 0.5, 2 or 4 h.

30986607
Immunofluorescence
p-STAT3 / p-ERK ; 

PubMed: 30986607     


Left, representative immunofluorescence of pSTAT3 (Y705) and pERK1/2 in U251/C7 cells treated with DMSO or cryptotanshinone (10 μM) for 4 h. Right, fluorescence intensity of pSTAT3 (Y705) (red box) and pERK1/2 (green box) in cells treated with or without Cryptotanshinone were quantified by ImageJ. Scale bar, 50 μm.

30986607
Growth inhibition assay
Cell viability; 

PubMed: 20820782     


The effect of Cryptotanshinone in different concentrations on B16 and B16BL6 melanoma cell growth.

20820782
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

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (16.87 mM)
Ethanol 1 mg/mL warmed (3.37 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
2mg/mL

* 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 Information

Molecular Weight 296.36
Formula

C19H20O3

CAS No. 35825-57-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID