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MedChemExpressModel Pyridostatin hydrochloride -1781882-65-2

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Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. 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].
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Pyridostatin hydrochloride

MCE China:Pyridostatin hydrochloride

Brand:MedChemExpress (MCE)

Cat. No.HY-15176A

CAS:1781882-65-2

Synonyms:RR82 hydrochloride

Purity:98.53%

Storage:4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. 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.

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].

IC50 & Target:Kd: 490 nM (G-quadruplexe)[1] 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Pyridostatin hydrochloride Related Antibodies Cell Viability Assay[1] Cell Line: Over 60 different cancer cell lines

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References:

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[4]. Zhang X, et al. Chemical profiling of DNA G-quadruplex-interacting proteins in live cells. Nat Chem. 2021 Jul;13(7):626-633.  [Content Brief]

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