Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer, with a Kd of 490 nM. Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. Pyridostatin (PDS) shows neurotoxic activity against primary cortical neurons at 0.01-5 μM, causes DNA double-strand breaks (DSBs) at 1 μM, downregulates BRCA1 in neurons at 1, 2 or 5 μM.
CAS# 1085412-37-8(free base)
|Cell lines||MRC-5–SV40 cells and various cancer cell lines|
|Preparation method||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.|
|Incubation time||48 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 90 mg/mL|
Small-molecule-induced DNA damage identifies alternative DNA structures in human genes.
Rodriguez R, et al. Nat Chem Biol. 2012 Feb 5;8(3):301-10. PMID: 22306580.
A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands.
Koirala D, et al. Nat Chem. 2011 Aug 28;3(10):782-7. PMID: 21941250.
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