RHPS 4 methosulfate

Catalog No.S8118 Batch:S811801

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Technical Data

Formula

C22H17F2N2.CH3O4S
Molecular Weight 458.48 CAS No. 390362-78-4
Solubility (25°C)* In vitro DMSO 91 mg/mL (198.48 mM)
Water Insoluble
Ethanol Insoluble
* <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.)

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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 (from reference)

Cell Assay:[2]
  • 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.
Animal Study:[2]
  • Animal Models

    CD-1 male nude (nu/nu) mice

  • Dosages

    15 mg/kg/d

  • Administration

    i.v.

Selleck's RHPS 4 methosulfate has been cited by 6 publications

Telomere as a Therapeutic Target in Dedifferentiated Liposarcoma [ Cancers (Basel), 2022, 14(11)2624] PubMed: 35681604
Monitoring and Modulating mtDNA G-Quadruplex Dynamics Reveal Its Close Relationship to Cell Glycolysis [ J Am Chem Soc, 2021, 143(49):20779-20791] PubMed: 34865478
Transcription-associated topoisomerase 2α (TOP2A) activity is a major effector of cytotoxicity induced by G-quadruplex ligands [ Elife, 2021, 10e65184] PubMed: 34180392
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] PubMed: 34771003
Melatonin Alleviates Age-Associated Endothelial Injury of Atherosclerosis via Regulating Telomere Function [ J Inflamm Res, 2021, 14:6799-6812] PubMed: 34924765
The TERT copy number gain is sensitive to telomerase inhibitors in human melanoma. [ Clin Sci (Lond), 2020, 10.1042/CS20190890] PubMed: 31919521

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.