Cryptotanshinone

Catalog No.S2285

For research use only.

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. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.

Cryptotanshinone Chemical Structure

CAS No. 35825-57-1

Selleck's Cryptotanshinone has been cited by 60 publications

Purity & Quality Control

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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. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
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
KB-3-1 NX;4fGY6S3m2b4TvfIlkcXS7IHHzd4F6 MnvQOFghcHK| M1;WR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGS{dXetd4Vve2m2aY\lJIh2dWGwIFvCMVMuOSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRUN1CPUzDhd5NigSxiSVO1NF03NjoQvF2= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd{MEWyNEc,OTF5MkC1NlA9N2F-
KBV1 NWTn[4N3S3m2b4TvfIlkcXS7IHHzd4F6 NXfLUXppPDhiaILz MnzRR5l1d3SxeHnjbZR6KGGpYXnud5QhdXWudHnkdpVoNXKnc3nzeIFvfCCqdX3hckBMSlZzIHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFNxUF3TJIF{e2G7LDDJR|UxRTdwNd88US=> M2TZWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzN{KwOVIxLz5zMUeyNFUzODxxYU6=
OVCAR-3 Mn7nR5l1d3SxeHnjbZR6KGG|c3H5 MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWi1|IHPlcIx{KGK7IF3UWEBie3OjeTygR2Q2OD17LkGy{txO MoLoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZyM{i1OVAoRjF4MEO4OVUxRC:jPh?=
HeLa NIq3[GtEgXSxdH;4bYNqfHliYYPzZZk> M2\xUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[nliTWTUJIF{e2G7LDDDSFUxRTF5LkNOwG0> M17xV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MEO4OVUxLz5zNkCzPFU2ODxxYU6=
HepG2 M2DkPGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{BjgSCPVGSgZZN{[XluIFPEOVA:OjlwN988US=> M{H2blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MEO4OVUxLz5zNkCzPFU2ODxxYU6=
Hep3B NVzsd4I5TnWwY4Tpc44h[XO|YYm= NUK5ZXNTOTZiaILz NYn2cJFSUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG2JIhzeyCkeTDy[ZBwenSncjDhd5NigSxiSVO1NF0yNjN4zszN Mn32QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
AGS MUHGeY5kfGmxbjDhd5NigQ>? NHvPWJAyPiCqcoO= NVW1dotzUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iQVfTJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzNjDodpMh[nlicnXwc5J1\XJiYYPzZZktKEmFNUC9NU42QM7:TR?= Mmj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
AGS MWLGeY5kfGmxbjDhd5NigQ>? NI[5OFkzPCCqcoO= NXvjVHV6XmmjYnnsbZR6KG:oIHj1cYFvKEGJUzDj[YxteyC3bnTldkBpgXCxeHnjJINwdmSrdHnvcpMh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNE4z|ryP MnPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
AGS NVftNpYzTnWwY4Tpc44h[XO|YYm= MV2yOEBpenN? MVjWbYFjcWyrdImgc4YhcHWvYX6gRWdUKGOnbHzzJJVv\GW{IH7vdo1wgGmlIHPvcoRqfGmxboOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zMz61{txO MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6M{m1NEc,OTd3OEO5OVA9N2F-
THLE3 MmT0R5l1d3SxeHnjbZR6KGG|c3H5 NFK4[5lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUEyHMzDj[YxteyCkeTDNWHQh[XO|YYmsJGVEPTB;MkKuPe69VQ>? NF;Xdoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MES1OVU4QCd-MkC0OVU2Pzh:L3G+
HepG2 MnzjRZBweHSxc3nzJIF{e2G7 MWXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJJA2OyCpZX7lJIF{e2W|c3XkJIF{KGOjc4Dhd4UhOyCjY4TpeoF1cW:w NFTnUIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MES1OVU4QCd-MkC0OVU2Pzh:L3G+
MIAPaCa2 NUPvfmtmS3m2b4TvfIlkcXS7IHHzd4F6 MWeyOEBpenN? NXWyWldkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13LklOwG0> NXPSTYNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3O|UyPTZpPkKxO|c2OTV4PD;hQi=>
HCT116 MlL4SpVv[3Srb36gZZN{[Xl? NILlSnEzPCCqcoO= NYjTZpRKUW6qaXLpeIlwdiCxZjDTWGFVOyCneIDy[ZN{\WRiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9OE43|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3MEOyOUc,OjJ4NUCzNlU9N2F-
BA/F3 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYm0PEBpenN? Mn3WS5Jwf3SqIHnubIljcXSrb36gc4YhUUx|LYP0bY12dGG2ZXSgcY92e2ViQlGvSlMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncjC5OkBie3OjeTygTWM2OD1zNz6yNu69VQ>? M1nSNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW3OFI3Lz5{M{m1O|QzPjxxYU6=
U-973 MlLDR4VtdCCleXPs[UBie3OjeR?= MYCxOUB1dyB|MDD1US=> MmTqNlQhcHK| NH3YNWJE\WyuIHP5Z4xmKGG{cnXzeEBifCCJMT3TJJBp[XOnIHnuJHBVWE5zMTDHOlBTKG23dHHueEBp[XKkb4LpcochcHWvYX6gWU06PzNiY3XscJMh[XRiMUWgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IF\BR3Mh[W6jbInzbZM> NIm4UFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m1O|QzPid-MkO5OVc1OjZ:L3G+
U-973 M2jkR2Fxd3C2b4Ppd{Bie3OjeR?= MoDxNVUhfG9iM{CgeW0> MWKyOEBpenN? MYLJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIGDUVG4yOSCJNkDSJI12fGGwdDDoZZJjd3KrbnegbJVu[W5iVT25O|Mh[2WubIOgZZQhOTVidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KE[DQ2OgZY5idHm|aYO= NYK4XI1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OVc1OjZpPkKzPVU4PDJ4PD;hQi=>
PTPN11 NIDibHBHfW6ldHnvckBie3OjeR?= NUPYTIx[OS53IITvJFYhfU1? NYrWT5E4OTRiZHH5dy=> NIi2fHdKdmirYnn0bY9vKG:oIFfNMWNUTi2rbnT1Z4VlKGe{b4f0bEBqdiCSVGDONVEhTTd4Sz:rJI16\WyxaXSgdJJw\2WwaYTvdkBk\WyuczDmdo9uKEqPTVygdIF1cWWwdDDheEAyNjVidH:gOkB2VSCjZoTldkAyPCCmYYnzJIJ6KGmwdnXyeIVlKG2rY4Lvd4NweGmlIHHuZYx6e2m| M2TJ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUW3OFI3Lz5{M{m1O|QzPjxxYU6=
PTPN11 M4WzSGZ2dmO2aX;uJIF{e2G7 MYSxMlUhfG9iNjD1US=> MXGxOEBl[Xm| MXTJcohq[mm2aX;uJI9nKEePLVPTSk1qdmS3Y3XkJINwdG:weTDmc5Ju[XSrb36gbY4hWFSSTkGxJGU4PktxKzDtfYVtd2mmIIDyc4dmdmm2b4KgZ4VtdHNiZoLvcUBLVU2OIIDheIlmdnRiYYSgNU42KHSxIE[geW0h[W[2ZYKgNVQh\GG7czDifUBqdn[ncoTl[EBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3N{SyOkc,OjN7NUe0NlY9N2F-
PTPN11 MYPGeY5kfGmxbjDhd5NigQ>? NETNZpQyNjVidH:gNVUhfU1? MVS3JIRigXN? NXjZSGJyUW6qaXLpeIlwdiCxZjDHUU1EW0ZvaX7keYNm\CClb3zvcpkh\m:{bXH0bY9vKGmwIGDUVG4yOSCHN{\LM{swVXiuLVPy[UshdW:3c3WgcZlmdG:rZDDwdo9o\W6rdH;yJINmdGy|IHH0JFEvPSC2bzCxOUB2VSCjZoTldkA4KGSjeYOgZpkhcW64ZYL0[YQhdWmlcn;zZ49xcWNiYX7hcJl{cXN? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3N{SyOkc,OjN7NUe0NlY9N2F-
HeLa MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV72eWVuOjRiaILz MV3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEK0JIhzew>? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3N{SyOkc,OjN7NUe0NlY9N2F-
Ba/F3 M3fXfmZ2dmO2aX;uJIF{e2G7 NUficFd6OzBidV2= MV2zJIhzew>? NWfLcIZQUW6qaXLpeIlwdiCxZjDJUFMucW6mdXPl[EBUUFB{LVfhZlIhcW62ZYLhZ5Rqd25iaX6gcY92e2ViQnGvSlMh[2WubIOgdJJmfHKnYYTl[EBifCB|MDD1UUBnd3JiMzDodpMheHKrb4KgTWw{KHO2aX31cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6pIH3leIhw\A>? NU\zZmQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OVc1OjZpPkKzPVU4PDJ4PD;hQi=>
SJ-GBM2 NWPxSWI2eUiWUzDhd5NigQ>? NVr5S4NpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> M{\qXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MVrxTHRUKGG|c3H5 NHSwSWVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MmjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-ERK / ERK 30986607
Immunofluorescence p-STAT3 / p-ERK 30986607
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[2]
  • 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

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG 300+5% Tween80 +ddH2O
For best results, use promptly after mixing.

1.25mg/mL

Chemical Information

Molecular Weight 296.36
Formula

C19H20O3

CAS No. 35825-57-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCCC4(C)C

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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