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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(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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|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, 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. 
|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. |
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.
|In vitro||DMSO||5 mg/mL warmed (16.87 mM)|
|Ethanol||1 mg/mL warmed (3.37 mM)|
|Water||slightly soluble or insoluble|
|In vivo||Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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