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）は、サブマイクロモルでテロメラーゼの強力な阻害剤です。
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.
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.

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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