Pyridostatin hydrochloride(Synonyms: RR82 hydrochloride)

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Pyridostatin hydrochloride (Synonyms: RR82 hydrochloride) 纯度: 98.77%

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。

Pyridostatin hydrochloride(Synonyms: RR82 hydrochloride)

Pyridostatin hydrochloride Chemical Structure

CAS No. : 1781882-65-2

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10 mM * 1 mL in Water ¥1268 In-stock
5 mg ¥1120 In-stock
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50 mg ¥6160 In-stock
100 mg ¥9380 In-stock
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Pyridostatin hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

778.94

Formula

C31H37Cl5N8O5

CAS 号

1781882-65-2

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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.

    [2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.

    [3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.

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