Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pyridostatin (RR82) 是一种 G-四链体稳定剂,靶向原癌基因 Src,降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。它通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Pyridostatin Trihydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 6-8周 | ||
5 mg | ¥ 720 | 6-8周 | ||
10 mg | ¥ 1,100 | 6-8周 | ||
25 mg | ¥ 1,950 | 6-8周 | ||
50 mg | ¥ 2,880 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 6-8周 |
Pyridostatin 的其他形式现货产品:
产品描述 | Pyridostatin (RR82) is a synthetic small-molecule stabilizer of G-quadruplexes, a secondary structure of DNA that usually exists in the end of the chromosome or the telomeres. |
靶点活性 | G-quadruplexe:490 nM(Kd) |
体外活性 | Pyridostatin decreases the proliferation of MRC-5–SV40 cells and various cancer cell lines, and induces cell-cycle arrest by DNA-damage checkpoint activation. Pyridostatin also reduces SRC-dependent cell motility in MDA-MB-231 cells by interacting with G-quadruplex motifs in SRC. [2] Pyridostatin decreases EBNA1 synthesis via inhibition of G-quadruplexes. [3] |
激酶实验 | Z-Lyte FRET kinase assay: Kinase inhibition is measured using the Invitrogen Z-Lyte? FRET kinase assay with Ser/Thr 13 peptide substrate based on the myosin light chain sequence KKRPQRRYSNVF. Compounds are tested on three separate days with 8 point dilutions performed in duplicate to determine average IC50 values. The assay conditions are optimized to 15 μL of kinase reaction volume with 5 ng of enzyme in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reaction is incubated for 1 h at room temperature in the presence of 1.5 μM of peptide substrate with 12.5 μM of ATP (for ROCK1) or 2 μM of substrate with 50 μM of ATP (for ROCK2). The reaction is then stopped and the ratio of phosphorylated to unphosphorylated peptides is determined by selective cleavage of only the unphosphorylated peptide as described by the manufacturer. This is followed by excitation of coumarin at 400 nm resulting in emission at 445 nm and energy transfer to fluorescein and final emission at 520 nm. The substrate contains both coumarin and fluorescein and only uncleaved phosphorylated substrate will undergo FRET. The ratio of the signals at 445 nm and 520 nm is measured using a Wallac EnVision Plate Reader, model 2102 plate-reader. |
细胞实验 | Cells are plated at equal confluence and are left either untreated or were treated with 2 μM pyridostatin continually during the indicated time before harvesting the cells. Cells from individual plates are trypsinized and counted in a Coulter counter. Graphs represent the total cell numbers at each time interval, and the error bars represent the s.e.m. Data represent three independent experiments.(Only for Reference) |
别名 | RR82, Pyridostatin Trifluoroacetate Salt |
分子量 | 596.64 |
分子式 | C31H32N8O5 |
CAS No. | 1085412-37-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20.85 mg/mL
Ethanol: 30.87 mg/mL, Heating is recommended.
H2O: 9.66 mg/mL, Sonication and heating are recommended.
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pyridostatin 1085412-37-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis DSB arrest neurodegeneration damage cycle SRC DNA G-quadruplex RR 82 RR82 RR-82 inhibit Inhibitor structure Pyridostatin Trifluoroacetate Salt inhibitor