research use only
Cat.No.S8118
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase |
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| Other Telomerase Inhibitors | BIBR 1532 Costunolide Cycloastragenol TAC (TERT Activator-1) Cyclogalegenol Braco-19 trihydrochloride L-778123 hydrochloride Epitalon MST-312 |
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In vitro |
DMSO
: 92 mg/mL
(200.66 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 458.48 | Formula | C22H17F2N2.CH3O4S |
Storage (From the date of receipt) | |
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| CAS No. | 390362-78-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC714187 | Smiles | CC1=CC2=C3C(=C1)N(C4=C(C3=[N+](C5=C2C=C(C=C5)F)C)C=C(C=C4)F)C.COS(=O)(=O)[O-] | ||
| Targets/IC50/Ki |
Telomerase
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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.
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| 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.
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References |
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