RHPS 4 methosulfate

For research use only.

Catalog No.S8118 Synonyms: NSC714187

3 publications

RHPS 4 methosulfate Chemical Structure

CAS No. 390362-78-4

RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar.

Selleck's RHPS 4 methosulfate has been cited by 3 publications

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Biological Activity

Description RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar.
Targets
Telomerase [1]
In vitro

RHPS4 triggers a rapid and potent DNA damage response at telomeres in human transformed fibroblasts and melanoma cells, characterized 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 delocalization of the protective telomeric DNA–binding protein POT1, and is antagonized by overexpression of POT1 or TRF2[2].

In vivo In mice, RHPS4 exerted its antitumor effect on xenografts of human tumor cells of different histotype by telomere injury and tumor cell apoptosis. Tumor inhibition was accompanied by a strong DNA damage response, and tumors overexpressing POT1 or TRF2 were resistant to RHPS4 treatment[2].

Protocol

Cell Research:[2]
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  • Cell lines: 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: CD-1 male nude (nu/nu) mice
  • Dosages: 15 mg/kg/d
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (198.48 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 458.48
Formula

C22H17F2N2.CH3O4S

CAS No. 390362-78-4
Storage powder
in solvent
Synonyms NSC714187
Smiles CC1=CC2=C3C(=C1)N(C4=C(C3=[N+](C5=C2C=C(C=C5)F)C)C=C(C=C4)F)C.COS(=O)(=O)[O-]

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID