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Synonyms | NSC714187 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H17F2N2.CH3O4S |
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分子量 | 458.48 | CAS No. | 390362-78-4 | |
Solubility (25°C)* | 体外 | DMSO | 92 mg/mL (200.66 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. |
製品説明 | RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar. |
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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]. |
細胞アッセイ | 細胞株 | Human transformed BJ-EHLT fibroblasts and M14 melanoma cells |
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濃度 | 1 μM | |
反応時間 | 3-8 hours | |
実験の流れ | 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. | |
動物実験 | 動物モデル | CD-1 male nude (nu/nu) mice |
投薬量 | 15 mg/kg/d | |
投与方法 | i.v. |
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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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。