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 58 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 Mme2R5l1d3SxeHnjbZR6KGG|c3H5 Mm\2OFghcHK| MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBlenWpLYPlcpNqfGm4ZTDoeY1idiCNQj2zMVEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UV{9RVVNiYYPzZZktKEmFNUC9Ok46|ryP M3nSfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzN{KwOVIxLz5zMUeyNFUzODxxYU6=
KBV1 NXzqN2pxS3m2b4TvfIlkcXS7IHHzd4F6 MmntOFghcHK| NXHjRmhFS3m2b4TvfIlkcXS7IHHnZYlve3RibYXseIllenWpLYLld4l{fGGwdDDoeY1idiCNQm[xJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOvVG1UKGG|c3H5MEBKSzVyPUeuOe69VQ>? NGTBOog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUeyNFUzOCd-MUG3NlA2OjB:L3G+
OVCAR-3 M{XDNWN6fG:2b4jpZ4l1gSCjc4PhfS=> NITpdINEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUj2zJINmdGy|IHL5JG1VXCCjc4PhfUwhS0R3ME25MlEz|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjB|OEW1NEc,OTZyM{i1OVA9N2F-
HeLa M1G0cGN6fG:2b4jpZ4l1gSCjc4PhfS=> MlLlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{BjgSCPVGSgZZN{[XluIFPEOVA:OTdwMt88US=> NFrS[YY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkCzPFU2OCd-MU[wN|g2PTB:L3G+
HepG2 MYrDfZRwfG:6aXPpeJkh[XO|YYm= MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{BjgSCPVGSgZZN{[XluIFPEOVA:OjlwN988US=> MnvVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZyM{i1OVAoRjF4MEO4OVUxRC:jPh?=
Hep3B NVP5NYNpTnWwY4Tpc44h[XO|YYm= M4D1clE3KGi{cx?= NUWzPYduUW6qaXLpeIlwdiCxZjDITWYyKGGldHn2ZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG2JIhzeyCkeTDy[ZBwenSncjDhd5NigSxiSVO1NF0yNjN4zszN MnnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
AGS MnPRSpVv[3Srb36gZZN{[Xl? NXHzb4pUOTZiaILz M4XMRWlvcGmkaYTpc44hd2ZiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBtfWOrZnXyZZNmKGW6cILld5Nqd25iYX\0[ZIhOTZiaILzJIJ6KHKncH;yeIVzKGG|c3H5MEBKSzVyPUGuOVjPxE1? M2PlfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUizPVUxLz5zN{W4N|k2ODxxYU6=
AGS MnPkSpVv[3Srb36gZZN{[Xl? M2fiNlI1KGi{cx?= MlvLWoli[mmuaYT5JI9nKGi3bXHuJGFIWyClZXzsd{B2dmSncjDofZBwgGmlIHPvcoRqfGmxboOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zMD6y{txO Mn7wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEO5OVAoRjF5NUizPVUxRC:jPh?=
AGS M3v0Z2Z2dmO2aX;uJIF{e2G7 NV\LT4FjOjRiaILz NV:2bZhoXmmjYnnsbZR6KG:oIHj1cYFvKEGJUzDj[YxteyC3bnTldkBvd3Kvb4jpZ{Bkd26maYTpc45{KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVMvPc7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6M{m1NEc,OTd3OEO5OVA9N2F-
THLE3 NHHReoZEgXSxdH;4bYNqfHliYYPzZZk> NIXROIhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUEyHMzDj[YxteyCkeTDNWHQh[XO|YYmsJGVEPTB;MkKuPe69VQ>? MkjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2NUW1O|goRjJyNEW1OVc5RC:jPh?=
HepG2 NU\KOnRqSXCxcITvd4l{KGG|c3H5 NHnMWGpKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDn[Y5mKGG|c3Xzd4VlKGG|IHPhd5Bie2ViMzDhZ5RqfmG2aX;u MlfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2NUW1O|goRjJyNEW1OVc5RC:jPh?=
MIAPaCa2 MUjDfZRwfG:6aXPpeJkh[XO|YYm= NXnSOJNlOjRiaILz MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQM7:TR?= M4HTfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{e1NVU3Lz5{MUe3OVE2PjxxYU6=
HCT116 M135c2Z2dmO2aX;uJIF{e2G7 MoPKNlQhcHK| NH3DdIFKdmirYnn0bY9vKG:oIGPURXQ{KGW6cILld5Nm\CCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME20MlbPxE1? NWPuPWd6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVA{OjVpPkKyOlUxOzJ3PD;hQi=>
BA/F3 NGP3fllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NG\CWGQ1QCCqcoO= MWfHdo94fGhiaX7obYJqfGmxbjDv[kBKVDNvc4TpcZVt[XSnZDDtc5V{\SCEQT;GN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{IEm2JIF{e2G7LDDJR|UxRTF5LkKy{txO NIPrfFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m1O|QzPid-MkO5OVc1OjZ:L3G+
U-973 NHzyNlJE\WyuIHP5Z4xmKGG|c3H5 MVqxOUB1dyB|MDD1US=> NIrOcZgzPCCqcoO= MWPD[YxtKGO7Y3zlJIFzemW|dDDheEBIOS2VIIDoZZNmKGmwIGDUVG4yOSCJNkDSJI12fGGwdDDoZZJjd3KrbnegbJVu[W5iVT25O|Mh[2WubIOgZZQhOTVidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KE[DQ2OgZY5idHm|aYO= NWP5eHkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OVc1OjZpPkKzPVU4PDJ4PD;hQi=>
U-973 M2CzZ2Fxd3C2b4Ppd{Bie3OjeR?= M375RVE2KHSxIEOwJJVO NE\EelgzPCCqcoO= MV3JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIGDUVG4yOSCJNkDSJI12fGGwdDDoZZJjd3KrbnegbJVu[W5iVT25O|Mh[2WubIOgZZQhOTVidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KE[DQ2OgZY5idHm|aYO= NYfZW4xxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OVc1OjZpPkKzPVU4PDJ4PD;hQi=>
PTPN11 MmrkSpVv[3Srb36gZZN{[Xl? MonlNU42KHSxIE[geW0> MXSxOEBl[Xm| M2LlV2lvcGmkaYTpc44hd2ZiR12tR3NHNWmwZIXj[YQh\3Kxd4ToJIlvKFCWUF6xNUBGPz[NLzugcZlmdG:rZDDwdo9o\W6rdH;yJINmdGy|IH\yc40hUk2PTDDwZZRq\W62IHH0JFEvPSC2bzC2JJVOKGGodHXyJFE1KGSjeYOgZpkhcW64ZYL0[YQhdWmlcn;zZ49xcWNiYX7hcJl{cXN? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl3N{SyOkc,OjN7NUe0NlY9N2F-
PTPN11 Mlv4SpVv[3Srb36gZZN{[Xl? NIHPTnQyNjVidH:gOkB2VQ>? MWCxOEBl[Xm| MmLhTY5pcWKrdHnvckBw\iCJTT3DV2YucW6mdXPl[EBkd2yxbomg[o9zdWG2aX;uJIlvKFCWUF6xNUBGPz[NLzugcZlmdG:rZDDwdo9o\W6rdH;yJINmdGy|IH\yc40hUk2PTDDwZZRq\W62IHH0JFEvPSC2bzC2JJVOKGGodHXyJFE1KGSjeYOgZpkhcW64ZYL0[YQhdWmlcn;zZ49xcWNiYX7hcJl{cXN? MmexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUe0NlYoRjJ|OUW3OFI3RC:jPh?=
PTPN11 NFvFdWtHfW6ldHnvckBie3OjeR?= NUDpclNXOS53IITvJFE2KHWP MnqyO{Bl[Xm| NFzNbVRKdmirYnn0bY9vKG:oIFfNMWNUTi2rbnT1Z4VlKGOxbH;ufUBnd3KvYYTpc44hcW5iUGTQUlEyKEV5NluvL{9OgGxvQ4LlL{Bud3W|ZTDtfYVtd2mmIIDyc4dmdmm2b4KgZ4VtdHNiYYSgNU42KHSxIEG1JJVOKGGodHXyJFch\GG7czDifUBqdn[ncoTl[EBucWO{b4Pjc5Bq[yCjbnHsfZNqew>? Mny5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUe0NlYoRjJ|OUW3OFI3RC:jPh?=
HeLa MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzmbVYzPCCqcoO= NFrKb|dIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFI1KGi{cx?= MnHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUe0NlYoRjJ|OUW3OFI3RC:jPh?=
Ba/F3 MoPjSpVv[3Srb36gZZN{[Xl? NXjjNIx1OzBidV2= MWmzJIhzew>? NXe0Nm1WUW6qaXLpeIlwdiCxZjDJUFMucW6mdXPl[EBUUFB{LVfhZlIhcW62ZYLhZ5Rqd25iaX6gcY92e2ViQnGvSlMh[2WubIOgdJJmfHKnYYTl[EBifCB|MDD1UUBnd3JiMzDodpMheHKrb4KgTWw{KHO2aX31cIF1cW:wIHL5JIludXWwb3Lsc5R1cW6pIH3leIhw\A>? MnS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NUe0NlYoRjJ|OUW3OFI3RC:jPh?=
SJ-GBM2 MXrxTHRUKGG|c3H5 NH;1XYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MlT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 M1fMWZFJXFNiYYPzZZk> MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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.
  • (Only for Reference)
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
  • (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):
5% DMSO+40%PEG 300+5% Tween80 +ddH2O
For best results, use promptly after mixing.

1.25mg/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 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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