Description
RHPS4 (NSC714187) is a potent inhibitor of Telomerase at submicromolar.
Product information
CAS Number: 390362-78-4
Molecular Weight: 458.48
Formula: C23H20F2N2O4S
Chemical Name: 4,16-difluoro-8,11,20-trimethyl-8,20-diazapentacyclo[11.7.1.0²,⁷.0⁹,²¹.0¹⁴,¹⁹]henicosa-1(20),2(7),3,5,9,11,13(21),14(19),15,17-decaen-20-ium methyl sulfate
Smiles: CC1C=C2C3=C(C=1)C1C=C(F)C=CC=1[N+](C)=C3C1C=C(F)C=CC=1N2C.COS([O-])(=O)=O
InChiKey: VRWGYMXWYZBBGF-UHFFFAOYSA-M
InChi: InChI=1S/C22H17F2N2.CH4O4S/c1-12-8-16-15-10-13(23)4-6-18(15)26(3)22-17-11-14(24)5-7-19(17)25(2)20(9-12)21(16)22;1-5-6(2,3)4/h4-11H,1-3H3;1H3,(H,2,3,4)/q+1;/p-1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C). 91 mg/mL(198.48 mM). Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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