Cryptotanshinone-Cryptotanshinon-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): STAT; Autophagy作通路: JAK/STAT Signaling; Stem Cell/Wnt; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 8.33 mg/mL (28.11 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)

3、先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (2.80 mM); Suspended solution; Need ultrasonic2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (2.80

4、mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 0.83 mg/mL (2.80 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Cryptotanshinone是從丹參的根中提取的天然化合物，具有抗腫瘤活性。 Cryptotanshinone抑制 STAT3 的IC50 為4.6 M。IC50 & Target STAT34.6 M (IC50)體外研究 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.體內(nèi)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 您邊的抑制劑師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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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