In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar concentrations.
Targets
Telomerase
In vitro
RHPS4 triggers a rapid and potent DNA damage response at telomeres in human transformed fibroblasts and melanoma cells, characterised by the formation of several telomeric foci containing phosphorylated DNA damage response factors γ-H2AX, RAD17, and 53BP1. This is dependent on DNA repair enzyme ATR, correlated with delocalisation of the protective telomeric DNA–binding protein POT1, and is antagonised by overexpression of POT1 or TRF2.
In Vivo
In mice, RHPS4 exerted its antitumour effect on xenografts of human tumour cells of different histotypes by telomere injury and tumour cell apoptosis. Tumour inhibition was accompanied by a strong DNA damage response, and tumours overexpressing POT1 or TRF2 were resistant to RHPS4 treatment.
Human transformed BJ-EHLT fibroblasts and M14 melanoma cells
Concentrations
1 μM
Incubation Time
3-8 hours
Method
RHPS4, used at a concentration of 1 μM for various times, is added to the cells 24 hours after plating. Cell counts and viability (trypan blue dye exclusion) are determined in each experiment. Caffeine at 10 mM, a dose with no toxic effect on cell viability, is left in the medium for 24 hours. Bleomycin is used at a concentration of 30 mM for 30 minutes.
Transcription-associated topoisomerase 2α (TOP2A) activity is a major effector of cytotoxicity induced by G-quadruplex ligands
[ Elife, 2021, 10e65184]
Studies on the Interactions of 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium and Insulin with the Quadruplex-Forming Oligonucleotide Sequence a2 from the Insulin-Linked Polymorphic Region
[ Molecules, 2021, 26(21)6595]
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SHIPPING AND STORAGE
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