RHPS 4 methosulfate

製品コードS8118 バッチS811801

印刷

化学情報

Chemical Structure Synonyms NSC714187 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H17F2N2.CH3O4S
分子量 458.48 CAS No. 390362-78-4
Solubility (25°C)* 体外 DMSO 91 mg/mL (198.48 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.

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生物活性

製品説明 RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human transformed BJ-EHLT fibroblasts and M14 melanoma cells
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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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