Home DNA Damage/DNA Repair Telomerase inhibitor RHPS 4 methosulfate For research use only.

RHPS 4 methosulfate

Synonyms: NSC714187

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

RHPS 4 methosulfate Chemical Structure

RHPS 4 methosulfate Chemical Structure

CAS No. 390362-78-4

Purity & Quality Control

RHPS 4 methosulfate Related Products

Signaling Pathway

Telomerase Signaling Pathways

Telomerase Signaling Pathway

Biological Activity

Description RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar.
Targets
Telomerase [1]
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models CD-1 male nude (nu/nu) mice
Dosages 15 mg/kg/d
Administration i.v.

Chemical Information & Solubility

Molecular Weight 458.48 Formula

C22H17F2N2.CH3O4S
CAS No. 390362-78-4 SDF Download RHPS 4 methosulfate SDF
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-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (200.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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