RHPS4
Based on 7 publication(s) in Google Scholar
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.
- Purity : 99.88%
- CAS No.: 390362-78-4
- Formula: C23H20F2N2O4S
- Molecular Weight:458.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) RHPS4
More- Nucleic Acids Res. 2025 Jan 7;53(1):gkae1259. [Abstract]
- J Exp Med. 2024 Nov 4;221(11):e20240435. [Abstract]
- Br J Pharmacol. 2025 Aug;182(16):3923-3951. [Abstract]
- Mol Cancer Ther. 2026 Jul 15:10.1158/1535-7163.MCT-26-0182.
- J Chem Inf Model. 2025 Jun 9;65(11):5718-5729. [Abstract]
- Antimicrob Agents Chemother. 2026 Oct 1:e0014426.
- bioRxiv. 2026 Jan 7.
Biological Activity
Description
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].
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RHPS4 (0.5-1 μM, 15 days) induces a senescent-like growth arrest in MCF-7 cells[1].
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RHPS4 (1 μM, 4 days) induces phosphorylation of H2AX in transformed and tumor cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, MCF-7 vector control, and MCF-7 c81 cells.
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Concentration:0, 0.2, 0.5, or 1 μM.
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Incubation Time:7 days.
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Result:Inhibited cell proliferation.
In Vivo
? 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:15 mg/kg.
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Administration:IV, daily for 15 consecutive days.
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Result:Active as a single agent on all the tumors analyzed. CG5 breast xenografts resulted in the most sensitive tumor.
Chemical Information
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CAS No. 390362-78-4
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Appearance Solid
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Molecular Weight 458.48
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Formula C23H20F2N2O4S
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Color Brown to reddish brown
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
A subcellular selective APEX2-based proximity labeling used for identifying mitochondrial G-quadruplex DNA binding proteins. [Abstract]2025 Jan 7;53(1):gkae1259. PMID: 39718986 -
J Exp Med
Inhibition of hTERT/telomerase/telomere mediates therapeutic efficacy of osimertinib in EGFR mutant lung cancer. [Abstract]2024 Nov 4;221(11):e20240435. PMID: 39297884 -
Br J Pharmacol
A mitochondria-targeting and G-quadruplex structure-binding ligand inducing calcium overload and ferroptosis in human cancer cells. [Abstract]2025 Aug;182(16):3923-3951. PMID: 40344208 -
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J Chem Inf Model
2025 Jun 9;65(11):5718-5729. PMID: 40366258 -
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Solvent & Solubility
In Vitro:
DMSO : 1 mg/mL (2.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (10.91 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jennifer C Cookson, et al. Pharmacodynamics of the G-quadruplex-stabilizing telomerase inhibitor 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in vitro: activity in human tumor cells correlates with telomere length and can be enhanced, or antagonized, with cytotoxic agents. Mol Pharmacol. 2005 Dec;68(6):1551-8. [Content Brief]
[2]. Erica Salvati, et al. Telomere damage induced by the G-quadruplex ligand RHPS4 has an antitumor effect. J Clin Invest. 2007 Nov;117(11):3236-47. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1811 mL | 10.9056 mL | 21.8112 mL | 54.5280 mL |