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Cryptotanshi

CAS No. : 35825-57-1

MCE 站：Cryptotanshi

产品活性：Cryptotanshi是从丹参的根中提取的天然化合物，具有抗肿瘤活性。 Cryptotanshi抑制 STAT3 的 IC₅₀ 为4.6 μM。

研究领域：JAK/STAT Signaling  |  Stem Cell/Wnt  |  Autophagy

作用靶点：STAT  |  Autophagy

In Vitro: Cryptotanshi significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705 phosphorylation ａnd the dimerization of STAT3, compared to tanshi IIA which exhibits no activity. Cryptotanshi (7 μM) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, ａnd significantly inhibits JAK2 phosphorylation with IC₅₀ of appr 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. Cryptotanshi 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. Cryptotanshi exhibits less growth inhibitory effect on PC3, LNCaP ａnd MDA-MB-468 cells. Cryptotanshi significantly attenuates the in vitro hormonal effects of DEX on ovaries, as indicated by a significant decrease in T ａnd an increase in P levels in the culture medium. Cryptotanshi significantly increases the levels of phosphorylated AKT2 ａnd GSK3β in the DEX-treated ovaries. Cotreatment with imatinib ａnd Cryptotanshi shows a significant synergistic killing effect in both imatinib sensitive ａnd resistant CML cell lines, as well as primary CML cells.

In Vivo: Cryptotanshi reverses the ovarian IR ａnd significantly increases 2-deoxy-D-[1,2-³H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshi significantly reduces the ovulation rate ａnd plasma E2 ａnd P levels. Cryptotanshi 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. Cryptotanshi 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 Cryptotanshi 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.

相关产品：Natural Product Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  Natural Product Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Diabetes Related Compound Library  |  Terpenoids Library  |  Traditional Chinese Medicine Monomer Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Transcription Factor Targeted Library  |  Food-Sourced Compound Library   |  Stattic  |  AG490  |  Fludarabine  |  AS1517499  |  Niclosamide  |  Artesunate  |  Homoharringtonine  |  TPCA-1  |  Colivelin TFA  |  NSC 74859  |  Napabucasin  |  Pimozide  |  C188-9  |  WP1066  |  STAT5-IN-1  |  AS2863619  |  Scutellarin  |  SH-4-54  |  SD-36  |  Cucurbitacin I  |  BP-1-102  |  Saikosaponin D  |  Nifuroxazide  |  STAT3-IN-1  |  Fraxinellone  |  Mogrol  |  Atractylenolide I  |  Dihydroisotanshi I  |  FLLL32  |  Alantolactone

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