1. Cell Cycle/DNA Damage
    Apoptosis
  2. Telomerase
    Apoptosis
  3. RHPS4

RHPS4 

Cat. No.: HY-101089
Handling Instructions

RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer.

For research use only. We do not sell to patients.

RHPS4 Chemical Structure

RHPS4 Chemical Structure

CAS No. : 390362-78-4

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Description

RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer[1][2].

IC50 & Target

IC50: 0.33 μM (telomerase in the TRAP assay)[1].

In Vitro

RHPS4 could sensitize tumor cells to anticancer agents that act via disparate mechanisms[1].
RHPS4 (0.5-1 μM, 15 days) induces a senescent-like growth arrest in MCF-7 cells[1].
RHPS4 (1 μM, 4 days) induces phosphorylation of H2AX in transformed and tumor cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MCF-7, MCF-7 vector control, and MCF-7 c81 cells.
Concentration: 0, 0.2, 0.5, or 1 μM.
Incubation Time: 7 days.
Result: Inhibited cell proliferation.
In Vivo

RHPS4 (15 mg/kg, iv, 15 days) treatment produces a marked inhibition of tumor weight (tumor weight inhibition [TWI] about 80%; P < 0.001) in a very short time, and this effect persists for at least 30 days. A complete tumor response is observed in 80% of mice, and 40% are cured[2].
In all the other tumor xenografts, RHPS4 treatment produces about 50% (P < 0.001) TWI at the nadir of the effect and, more important, results in a delay of tumor growth of about 15 (M14 and PC3) and 10 (HT29 and H460) days[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 male nude (nu/nu) mice, 6–8 weeks old and weighing 22-24 g (H460, CG5 and HT29, PC3 and M14 cancer models)[2].
Dosage: 15 mg/kg.
Administration: IV, daily for 15 consecutive days.
Result: Active as a single agent on all the tumors analyzed. CG5 breast xenografts resulted in the most sensitive tumor.
Molecular Weight

458.48

Formula

C₂₃H₂₀F₂N₂O₄S

CAS No.
SMILES

O=S([O-])(OC)=O.FC1=CC=C2C(C3=[N+](C)C4=C(C=C(C=C4)F)C5=C3C(N2C)=CC(C)=C5)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RHPS4RHPS 4RHPS-4TelomeraseApoptosisH460CG5HT29PC3M14breastcancerH2AXInhibitorinhibitorinhibit

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