Cryptotanshinone是从丹参的根中提取的一种天然产物，抑制STAT3的IC50为4.6 μM，具有抗肿瘤活性。

Cryptotanshinone, a STAT3 inhibitor (IC50: 4.6 μM) in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a little effect on STAT3 Ser727, but no inhibition for STAT1 nor STAT5.

在ob/ob小鼠 (C57BL/6J-Lepob)、db/db 小鼠(C57BL/KsJ-Leprdb)和ZDF大鼠体内,经Cryptotanshinone（600 mg/kg/day）3天处理,可使血糖水平显著降低,且在监测期内一直维持降低水平.在ob/ob小鼠(C57BL/6J-Lepob) 和饮食导致的肥胖小鼠中,Cryptotanshinone剂量依赖性地显著降低体重和食物摄入.Cryptotanshinone可使脂肪组织的脂肪明显降低,并显著降低血清胆固醇和甘油三酯水平,且骨骼肌中, AMPK活性比对照组小鼠高2.5-3倍.

在DU145细胞中,Cryptotanshinone（7 μM）处理30 min,对STAT3在Tyr705位点的磷酸化有显著抑制效果,但不影响STAT3在Ser727位点磷酸化,处理4小时后,对JAK2 磷酸化有明显抑制作用（IC50：5 μM）,但对下游激酶c-Src和EGFR的磷酸化无影响,表明抑制STAT3在Tyr705位点磷酸化是因为与STAT3的SH2域结合。Cryptotanshinone是分离自丹参根中的天然产物,对STAT3依赖的荧光素酶活性有显著抑制作用,且抑制STAT3在Tyr705位点磷酸化及STAT3二聚体化。Cryptotanshinone对含组成型激活STAT3的DU145细胞系增殖有显著抑制效果（GI50：7 μM）,可阻断STAT3活性,从而下调cyclin D1、Bcl-xL和凋亡抑制基因,随后使细胞在G0-G1期累积。Cryptotanshinone对PC3、LNCaP和MDA-MB-468细胞的生长有微弱抑制作用。

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.

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.(Only for Reference)

35825-57-1

C19H20O3

296.37

隐丹参酮;隐丹参醌;Tanshinone c;Cryptotanshinon

DMSO:3 mg/mL (10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years