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.

Size Price Stock Quantity  
In DMSO USD 70 In stock
USD 50 In stock
USD 110 In stock
USD 210 In stock

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1 Customer Review

  • A. A2780 and ES2 cells were treated with different concentrations of STAT3 inhibitor, Cryptotanshinone (0, 0.5, 1, 1.5 μM for A2780 cells and 0, 20, 40, 60 μM for ES2 cells) for 24 h. Then the expression level of p-STAT3, STAT3, Bcl-2 and Survivin were analyzed by Western blotting.

    Biochem Biophys Res Commun, 2016, 470(4):947-54.. Cryptotanshinone purchased from Selleck.

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
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 Mk[zSpVv[3Srb36gZZN{[Xl? NF;POJMyPiCq NXy5RVF3UW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG2JIhzeyCkeTDy[ZBwenSncjDhd5NigSxiSVO1NF0yNjN4IN88US=> NIP0bXUyPzV6M{m1NC=>
human AGS cells MWjGeY5kfGmxbjDhd5NigQ>? MkTkNVYhcA>? NV31bmdvUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iQVfTJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzNjDodpMh[nlicnXwc5J1\XJiYYPzZZktKEmFNUC9NU42QCEQvF2= NHPRUYYyPzV6M{m1NC=>
human HCT116 cells MVfGeY5kfGmxbjDhd5NigQ>? MYKyOEBp M4nvTmlvcGmkaYTpc44hd2ZiU2TBWFMh\XiycnXzd4VlKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBq[zVyPUSuOkDPxE1? NVG3bWNQOjJ4NUCzNlU>
human MIAPaCa2 cells NVnuO4s5S3m2b4TvfIlkyqCjc4PhfS=> Mn7vNlQhcA>? MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2= M4HSd|IyPzd3MUW2
human KB-3-1 cells NWO3VnZTS3m2b4TvfIlkyqCjc4PhfS=> M3:2e|Q5KGh? NXu4fFZbS3m2b4TvfIlkcXS7IHHnZYlve3RiZIL1[{1{\W6|aYTpeoUhcHWvYX6gT2IuOy1zIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFNxUF3TJIF{e2G7LDDJR|UxRTZwOTFOwG0> M2PJeFEyPzJyNUKw
human KBV1 cells MoXsR5l1d3SxeHnjxsBie3OjeR?= NHfnfpI1QCCq MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBufWy2aXTyeYcuemW|aYP0ZY51KGi3bXHuJGtDXjFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VWy:STWOgZZN{[XluIFnDOVA:Py53IN88US=> MYexNVczODV{MB?=
human AGS cells MmD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYL4Z3NMOjRiaB?= NGT1OFZXcWGkaXzpeJkhd2ZiaIXtZY4hSUeVIHPlcIx{KHWwZHXyJIh6eG:6aXOgZ49v\Gm2aX;ud{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGwMlIh|ryP NXzMS5g1OTd3OEO5OVA>
human THLE3 cells M1nDSGN6fG:2b4jpZ:Kh[XO|YYm= MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUTGxGOyClZXzsd{BjgSCPVGSgZZN{[XluIFXDOVA:OjJwOTFOwG0> MlfpNlA1PTV3N{i=
human PBMC Mnn0SpVv[3Srb36gZZN{[Xl? MmnETY5pcWKrdHnvckBw\iCyaIn0c4hmdWGpZ3z1eIlvcW6rbjDBMZN1cW23bHH0[YQhcHWvYX6gVGJOSyCycn;sbYZmemG2aX;uJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIGuxOGNefGi7bXnkbY5mKGmwY3;ydI9z[XSrb36sJGlEPTB;M{euOEDPxE1? MYGxNVczODV{MB?=
PTPN11 E76K/+ MEF NEHnZVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIjyWWYzOCEQvF2= MYnHdo94fGhiaX7obYJqfGmxbjDv[kBRXFCQMUGgSVc3Uy9tIF3FSkBifCB{MDD1US=> M2jnUVI{QTV5NEK2
human HeLa cells NH7KcGpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUmyOEBp M4DFT2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgNlQhcHK| NVflfGQzOjN7NUe0NlY>
human HepG2 cells Mo[yR5l1d3SxeHnjxsBie3OjeR?= NHrxV|lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCkeTDNWHQh[XO|YYm= NF7sNo8yPjB|OEW1NC=>
human OVCAR-3 cells NX7RN4dwS3m2b4TvfIlkyqCjc4PhfS=> MnXYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJvMzDj[YxteyCkeTDNWHQh[XO|YYm= NHXVS2syPjB|OEW1NC=>
mouse Ba/F3 cells MYTGeY5kfGmxbjDhd5NigQ>? M{DNTVMxKM7:TR?= NFn0XVU{KGh? NX3DVFZ1UW6qaXLpeIlwdiCxZjDJUFMucW6mdXPl[EBUUFB{LVfhZlIhcW62ZYLhZ5Rqd25iaX6gcY92e2ViQnGvSlMh[2WubIOgdJJmfHKnYYTl[EBifCB|MDD1UUBnd3JiMzDodpMheHKrb4KgTWw{KHO2aX31cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6pIH3leIhw\A>? MX2yN|k2PzR{Nh?=

... Click to View More Cell Line Experimental Data

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]


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 <1 mg/mL
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 Information

Molecular Weight 296.36


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID