Cryptotanshinone-Cryptotanshinon-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECryptotanshinoneCat. No.: HY-N0174CAS No.: 35825-57-1Synonyms: Cryptotanshinon; Tanshinone c分式: CHO分量: 296.36作靶点: STAT; Autophagy作通路: JAK/STAT Signaling; Stem Cell/Wnt; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性数据体外实验 DMSO : 8.33 mg/mL (28.11 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3743 mL 16.8714 mL 33.7427 mL5 mM 0.6749 mL 3.3743 mL 6.7485 mL10 mM 0.3374 mL 1.6871 mL 3.3743 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请

3、先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (2.80 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (2.80

4、mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 0.83 mg/mL (2.80 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Cryptotanshinone是从丹参的根中提取的天然化合物，具有抗肿瘤活性。 Cryptotanshinone抑制 STAT3 的IC50 为4.6 M。IC50 & Target STAT34.6 M (IC50)体外研究 Cryptotansh

5、inone significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705phosphorylation and the dimerization of STAT3, compared to tanshinone IIA which exhibits no activity.Cryptotanshinone (7 M) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727phosphorylation in DU145

6、cells, and significantly inhibits JAK2 phosphorylation with IC50 of appr 5 Mwithout affecting the phosphorylation of upstream kinases c-Src and EGFR, suggesting the inhibition ofSTAT3 Tyr705 phosphorylation might due to a direct mechanism probably by binding to the SH2 domain ofSTAT3. Cryptotanshino

7、ne significantly inhibits the proliferation of DU145 prostate cancer cells harboringconstitutively active STAT3 with GI50 of 7 M by blocking STAT3 activity, which leads to the down-regulationof cyclin D1, Bcl-xL, and survivin, subsequently the accumulation in the G0-G1 phase. Cryptotanshinoneexhibit

8、s less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells 1. Cryptotanshinonesignificantly attenuates the in vitro hormonal effects of DEX on ovaries, as indicated by a significant decreasein T and an increase in P levels in the culture medium. Cryptotanshinone significantly increases the l

9、evels ofphosphorylated AKT2 and GSK3 in the DEX-treated ovaries 2. Cotreatment with imatinib andCryptotanshinone shows a significant synergistic killing effect in both imatinib sensitive and resistant CMLcell lines, as well as primary CML cells 3.体内研究 Cryptotanshinone reverses the ovarian IR and sig

10、nificantly increases 2-deoxy-D-1,2-3H-glucose uptake inall examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rateand plasma E2 and P levels 2. Cryptotanshinone administration significantly reduces the body weight andfood intake of ob/ob mice (C57BL/6J-L

11、epob) and diet-induced obese (DIO) mice in a dose-dependentmanner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serumtriglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in thecontrol mice. Oral ad

12、ministration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions inblood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, whichoccur after 3 days and persist over the entirety of the monitoring period 4.PROTOCOLKinase Assay 1 HCT-116 cells are

13、 transiently transfected with reporter plasmid having the STAT3-binding element forregulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of0.2 to 50 M. After treatment, cells are harvested in 20 L of passive lysis buffer and luciferase activity is

14、evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of2/3 Master of Small Molecules 您边的抑制剂师www.MedChemECryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.MCE has not independently confirmed the accuracy of these methods. They are

15、for reference only.Cell Assay 3 The MTT assay is used for the assessment of cell growth inhibition as described previously. Cells are seededat a density of 8000 cells per well in 96-well plates in RPMI-1640 containing 10% FBS. Differentconcentrations of imatinib and CPT are added and incubated for a

16、nother 24 h. Then, 20 L of MTT areadded into each well and the absorbance at 570 nm is measured on an enzyme linked immunosorbent assay(ELISA) plate reader. The coefficient of drug interaction (CDI) between imatinib and CPT is determinedaccording to a previous study. The calculated method is as foll

17、ows: CDI/AB/(A B). According to theabsorbance of each group, AB is the ratio of the combination group to the control group; A or B is the ratio ofthe single agent group to the control group. CDI 1 indicates an antagonistic effect. In the combination treatment group, the concentrations ofCPT are arbi

18、trarily designated according to the 50% inhibitory concentration (IC50) value. Then, the cellviabilities are determined after treatment with different concentrations of imatinib plus CPT (constant CPTconcentration for one cell type). Finally, the combination IC50 values of imatinib are calculated, a

19、nd arerepresented in Table I. The primary CML cells CP1 to CP3 are isolated from patients in chronic phase, whileBC1 and BC2 are isolated from patients in blast crisis. Three independent sets of experiments areperformed. The IC50 values are presented as the meanstandard deviation (SD).MCE has not in

20、dependently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Pineal Res. 2019 Apr;66(3):e12552. PLoS Genet. 2015 Mar 27;11(3):e1005120. J Cell Mol Med. 2017 Sep;21(9):2172-2183. Sci Rep. 2016 Dec 6;6:38408. Am J Transl Res. 2016 Sep 15;8(9):3848-3860.See more custom

21、er validations on HYPERLINK / www.MedChemEREFERENCES1. Shin DS, et al. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking thedimerization in DU145 prostate cancer cells. Cancer Res. 2009 Jan 1;69(1):193-202.2. Huang Y, et al. Cryptotanshinone reverses ovarian insulin resistance in mice