Cryptotanshinone是一种从丹参的根中提取的天然化合物,抑制 STAT3 的 IC50 为4.6 μM,具有潜在的抗肿瘤活性。
别名:CTS
Cryptotanshinone was originally isolated from the dried roots of Salvia militorrhiza, an herb that is used extensively in Asian medicine and that is known to exert beneficial effects on the circulatory system.Cryptotanshinone rapidly inhibited STAT3 Tyr705 phosphorylation in DU145 prostate cancer cells and the growth of the cells through 96 hours of the treatment.Cryptotanshinone significantly attenuated atherosclerotic plaque formation and enhanced plaque stability in ApoE-/- mice by inhibiting lectin-like oxLDL receptor-1 (LOX-1) and matrix metalloproteinase-9 (MMP-9) expression, as well as inhibiting reactive oxygen species (ROS) generation and nuclear factor- kappa B (NF-κB) activation.In vitro,Cryptotanshinone decreased oxLDL-induced LOX-1 mRNA and protein expression, and thereby, inhibited LOX-1-mediated monocytes adhesion to HUVECs through reducing the expression of adhesion molecules (ICAM-1 and VCAM-1).Cryptotanshinone inhibited NADPH oxidase subunit 4 (NOX4)-mediated ROS generation and consequent activation of NF-κB in HUVECs.
Inflammation. 2023 Oct 7.
Front Immunol. 2022 Feb 7;13:820685.
Acta Pharmacol Sin. 2019 Dec 17.
Acid sphingomyelinase downregulation alleviates vascular endothelial leptin resistance in rats.
体外实验* | |
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细胞系 | KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116 |
方法 | Exposing cells to Cryptotanshinone for 24 or 48 hours. For the determination of cell proliferation, adding the cell proliferation reagent WST-1 and using an ELISA reader to measure WST-1 formazan quantitatively at 450 nm. |
浓度 | Dissolved in DMSO, final concentrations ~50 μM |
处理时间 | 24 or 48 hours |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | 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 |
配制 | Dissolved in 0.1% solution of sodium lauryl sulfate |
剂量 | ~600 mg/kg/day |
给药处理 | Orally |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 296.36 |
分子式 | C19H20O3 |
CAS号 | 35825-57-1 |
溶解性(25°C) | DMSO 3 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.3743 mL | 16.8714 mL | 33.7427 mL |
5 mM | 0.6749 mL | 3.3743 mL | 6.7485 mL |
10 mM | 0.3374 mL | 1.6871 mL | 3.3743 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
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