product name RHPS4
Description: RHPS4 (also known as NSC714187) is a potent inhibitor of Telomerase at submicromolar. Treatment of UXF1138L cells with RHPS4 led to the displacement of the telomerase catalytic subunit (hTERT) from the nucleus, induction of telomere-initiated DNA-damage signalling as well as chromosome fusions. It was further reported that RHPS4 was more potent over cancer cells growing as colonies than cells growing as monolayers.
References: Br J Cancer. 2007 Apr 23;96(8):1223-33; J Clin Invest. 2007 Nov;117(11):3236-47.
458.48
Formula
C22H17F2N2.CH3O4S
CAS No.
390362-78-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 91 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
NSC714187
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: 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. Cell lines used: Human transformed BJ-EHLT fibroblasts and M14 melanoma cells |
|---|---|
| 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. |
| Animal model | CD-1 male nude (nu/nu) mice |
| Formulation & Dosage | Dissolved in saline; 15 mg/kg/d; i.v. injection |
| References | Br J Cancer. 2007 Apr 23;96(8):1223-33; J Clin Invest. 2007 Nov;117(11):3236-47. |
