RHPS 4 methosulfate

製品コードS8118 バッチS811803

印刷

化学情報

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

92 mg/mL (200.66 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4mg/ml (8.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

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.

参考

https://pubmed.ncbi.nlm.nih.gov/17406367/
https://pubmed.ncbi.nlm.nih.gov/17932567/

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：

Naphthalene diimide-naphthalimide dyads promote telomere damage by selectively targeting multimeric G-quadruplexes [ Nucleic Acids Res, 2025, 53(7)gkaf301]	PubMed: 40239997
Genomic context influences translesion synthesis DNA polymerase-dependent mechanisms of micronuclei induction by G-quadruplexes [ Cell Rep, 2025, 44(5):115706]	PubMed: 40349342
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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