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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3 Customer Reviews

  • (a) Effect on STAT3 DNA binding activity of the STAT3 inhibitors cryptotanshinone (CTN) and S31-201 in STAT3 mutant cell lines OCI-Ly12 and OCI-Ly13.2. (b) Effect on cell viability at 48 h of the STAT3 inhibitors cryptotanshinone and S31-201 in OCI-Ly12 and OCI-Ly13.2 cells.

    Nat Commun, 2017, 8:14290. Cryptotanshinone purchased from Selleck.

    a. Changes in the expression of p-STAT3, p-ERK1/2, p-AKT, STAT3, p-ERK1/2 and AKT according to Western blotting. p-STAT3 and p-ERK1/2 were detected during the first 30 min of rhIL-6 treatment, indicating that rhIL-6 activated the JAK/STAT3 and MAPK/ERK1/2 pathways but not the PI3K/AKT pathway. b. MTT assay for F5M2 cells treated with different concentrations of the STAT3 inhibitor cryptotanshinone or the ERK1/2 inhibitor FR180204. Both inhibitors reduced F5M2 cell proliferation compared with the control DMSO (P < 0.001). Cryptotanshinone had a substantially greater inhibitory effect than FR180204 (P < 0.001). ED50cryptotanshinone=19.03 μM and ED50FR180204=89.20 μM. c. Pre-treatment of F5M2 cells with 50 μM cryptotanshinone prior to rhIL-6 incubation effectively reduced p-STAT3 levels. d. Pre-treatment of F5M2 cells with 2 μM FR180204 prior to rhIL-6 incubation effectively reduced p-ERK1/2 expression.

    Oncotarget, 2016, 7(1):446-58. Cryptotanshinone purchased from Selleck.

  • 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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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 NV;KZXU4TnWwY4Tpc44h[XO|YYm= NGXEclQyPiCq MYLJcohq[mm2aX;uJI9nKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBJ\XB|QjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBtfWOrZnXyZZNmKGW6cILld5Nqd25iYX\0[ZIhOTZiaILzJIJ6KHKncH;yeIVzKGG|c3H5MEBKSzVyPUGuN|Yh|ryP NVrXeZhLOTd3OEO5OVA>
human AGS cells MWLGeY5kfGmxbjDhd5NigQ>? NXPT[XkyOTZiaB?= MkPjTY5pcWKrdHnvckBw\iCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hSUeVIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmyb4jpZU1qdmS3Y3XkJIx2[2moZYLhd4Uh\XiycnXzd4lwdiCjZoTldkAyPiCqcoOgZpkhemWyb4L0[ZIh[XO|YYmsJGlEPTB;MT61PEDPxE1? M{H4VlE4PTh|OUWw
human HCT116 cells M{DOXmZ2dmO2aX;uJIF{e2G7 M4DuSlI1KGh? NG\HRVFKdmirYnn0bY9vKG:oIGPURXQ{KGW6cILld5Nm\CCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhcWN3ME20MlYh|ryP MY[yNlY2ODN{NR?=
human MIAPaCa2 cells Mor6R5l1d3SxeHnjxsBie3OjeR?= NVXhbXppOjRiaB?= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2= MUGyNVc4PTF3Nh?=
human KB-3-1 cells M4rXeGN6fG:2b4jpZ:Kh[XO|YYm= M37IW|Q5KGh? MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBlenWpLYPlcpNqfGm4ZTDoeY1idiCNQj2zMVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UV{9RVVNiYYPzZZktKEmFNUC9Ok46KM7:TR?= NXq5UWNTOTF5MkC1NlA>
human KBV1 cells MX\DfZRwfG:6aXRCpIF{e2G7 MX20PEBp MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBufWy2aXTyeYcuemW|aYP0ZY51KGi3bXHuJGtDXjFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VWy:STWOgZZN{[XluIFnDOVA:Py53IN88US=> NIm3XGYyOTd{MEWyNC=>
human AGS cells M4HwRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHSXVYzPCCq M3naUnZq[WKrbHn0fUBw\iCqdX3hckBCT1NiY3XscJMhfW6mZYKgbJlxd3irYzDjc45lcXSrb37zJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUCuNkDPxE1? MVuxO|U5Ozl3MB?=
human THLE3 cells MUTDfZRwfG:6aXRCpIF{e2G7 Mln3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWGhNTTNiY3XscJMh[nliTWTUJIF{e2G7LDDFR|UxRTJ{Lkmg{txO NWjaclc5OjB2NUW1O|g>
human PBMC M1;DVmZ2dmO2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKHCqeYTvbIVu[WepbIX0bY5qdmmwIFGtd5RqdXWuYYTl[EBpfW2jbjDQRm1EKHC{b3zp[oVz[XSrb36gZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iW{G0R311cHmvaXTpcoUhcW6lb4Lwc5JifGmxbjygTWM2OD1|Nz60JO69VQ>? MYKxNVczODV{MB?=
PTPN11 E76K/+ MEF M3jKWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\CdlIxKM7:TR?= MojzS5Jwf3SqIHnubIljcXSrb36gc4YhWFSSTkGxJGU4PktxKzDNSWYh[XRiMkCgeW0> M3XlWVI{QTV5NEK2
human HeLa cells NGDiRnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX6yOEBp NELKO|lIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFI1KGi{cx?= MlvuNlM6PTd2Mk[=
human HepG2 cells NU\IbGhlS3m2b4TvfIlkyqCjc4PhfS=> NETvXVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCkeTDNWHQh[XO|YYm= MmrkNVYxOzh3NUC=
human OVCAR-3 cells NEnvSlNEgXSxdH;4bYPDqGG|c3H5 Mn\DR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJvMzDj[YxteyCkeTDNWHQh[XO|YYm= NX;kdpRzOTZyM{i1OVA>
mouse Ba/F3 cells NXfN[W1wTnWwY4Tpc44h[XO|YYm= MVyzNEDPxE1? NILTd5Y{KGh? NHuxfolKdmirYnn0bY9vKG:oIFnMN{1qdmS3Y3XkJHNJWDJvR3HiNkBqdnSncnHjeIlwdiCrbjDtc5V{\SCEYT;GN{Bk\WyuczDwdoV1emWjdHXkJIF1KDNyIIXNJIZweiB|IHjyd{BxemmxcjDJUFMhe3SrbYXsZZRqd25iYomgbY1ufW6xYnzveJRqdmdibXX0bI9l M3LZb|I{QTV5NEK2

... 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]

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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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.

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:

    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