受注:045-509-1970 |
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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H20O3 |
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分子量 | 296.36 | CAS No. | 35825-57-1 | |
Solubility (25°C)* | 体外 | DMSO | 9 mg/mL warmed with 50ºC water bath (30.36 mM) | |
Ethanol | 4 mg/mL warmed with 50ºC water bath (13.49 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | Cryptotanshinone (Tanshinone C) 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. |
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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] |
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] |
キナーゼアッセイ | STAT3-dependent dual-luciferase assay | |
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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. | ||
細胞アッセイ | 細胞株 | KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116 |
濃度 | Dissolved in DMSO, final concentrations ~50 μM | |
反応時間 | 24 or 48 hours | |
実験の流れ | 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. | |
動物実験 | 動物モデル | 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 |
投薬量 | ~600 mg/kg/day | |
投与方法 | Orally |
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Data from [Data independently produced by , , Nat Commun, 2017, 8:14290]
Data from [Data independently produced by , , Diabetes, 2018, 67(2):235-247]
Data from [Data independently produced by , , Cancer Lett, 2018, 416:24-30]
Revisiting the role of endogenous STAT3 in HPV-positive cervical cancer cells [ J Med Virol, 2023, 95(11):e29230] | PubMed: 38009614 |
Galectin-9 Facilitates Epstein-Barr Virus Latent Infection and Lymphomagenesis in Human B Cells [ Microbiol Spectr, 2023, e0493222.] | PubMed: 36622166 |
Inhibitory Effect and Mechanism of Ursolic Acid on Cisplatin-Induced Resistance and Stemness in Human Lung Cancer A549 Cells [ Evid Based Complement Alternat Med, 2023, 2023:1307323] | PubMed: 37089712 |
Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632] | PubMed: 37828768 |
Bile Acid-Microbiome Interaction Promotes Gastric Carcinogenesis [ Adv Sci (Weinh), 2022, e2200263] | PubMed: 35285172 |
B7-H4 expression is upregulated by PKCδ activation and contributes to PKCδ-induced cell motility in colorectal cancer [ Cancer Cell Int, 2022, 22(1):147] | PubMed: 35410218 |
The endosomal pH regulator NHE9 is a driver of stemness in glioblastoma [ PNAS Nexus, 2022, 1(1):pgac013] | PubMed: 35387234 |
USP24-GSDMB complex promotes bladder cancer proliferation via activation of the STAT3 pathway [ Int J Biol Sci, 2021, 17(10):2417-2429] | PubMed: N/A |
The Antimicrobial Peptide Human β-Defensin-3 Accelerates Wound Healing by Promoting Angiogenesis, Cell Migration, and Proliferation Through the FGFR/JAK2/STAT3 Signaling Pathway [ Front Immunol, 2021, 12:712781] | PubMed: 34594328 |
TTI-101: A competitive inhibitor of STAT3 that spares oxidative phosphorylation and reverses mechanical allodynia in mouse models of neuropathic pain [ Biochem Pharmacol, 2021, 192:114688] | PubMed: 34274354 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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