Pyridostatin (RR82) hydrochloride 是一种高选择性的G-quadruplex DNA稳定剂 (Kd=490 nM)。Pyridostatin hydrochloride 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。Pyridostatin hydrochloride 靶向原癌基因 Src。Pyridostatin hydrochloride 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。
生物活性 | Pyridostatin (RR82) hydrochloride is aG-quadruplexDNAstabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in humancancercells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogeneSrc. Pyridostatin hydrochloride reducedSRCprotein levels and SRC-dependent cellular motility in human breastcancercells[1][2]. |
IC50& Target | Kd: 490 nM (G-quadruplexe)[1] |
体外研究 (In Vitro) | Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin hydrochloride is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin hydrochloride causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin hydrochloride induces the formation of DNA DSBs. Remarkably, Pyridostatin hydrochloride (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3].
Cell Viability Assay[1] Cell Line: | Over 60 different cancer cell lines | Concentration: | 10 μM | Incubation Time: | 48 hours | Result: | Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: H2O : 50 mg/mL(64.19 mM;Need ultrasonic) 配制储备液 1 mM | 1.2838 mL | 6.4190 mL | 12.8380 mL | 5 mM | 0.2568 mL | 1.2838 mL | 2.5676 mL | 10 mM | 0.1284 mL | 0.6419 mL | 1.2838 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (128.38 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |