RHPS4

RHPS4

Catalog Number:
L002371490APE
Mfr. No.:
APE-B6186
Price:
$375
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      • Overview
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          Background

          IC50: ~3 μM for M14 cells in 5-day growth inhibition assayRHPS4 is a telomerase inhibitor.The protection of chromosome termini, degradation and recombination is regulated by the telomeres. A recent model proposes that telomeres can form a cap at the chromosome end. Thus, the telomere cap integrity should be intact to allow cell division to proceed.In vitro: It was found that the treatment RHPS4 to UXF1138L cells led to the displacement of the telomerase catalytic subunit (hTERT) from the nucleus, induction of telomere-initiated DNA-damage signalling as well as chromosome fusions. It was further reported that RHPS4 was more potent over cancer cells growing as colonies than cells growing as monolayers. In addition, the forming units of human cord blood and HEK293T embryonic kidney cell colony were more resistant to RHPS4 [1]. In vivo: Animal study found that, compared with controls, RHPS4-treated UXF1138L xenografts had a decreased clonogenicity, loss of nuclear hTERT expression and an induction of mitotic abnormalities. Though RHPS4 alone showed limited in vivo efficacy, a combination treatment with the mitotic spindle poison Taxol resulted in tumour remissions and further enhancement of telomere dysfunction [1]. Clinical trial: Up to now, RHPS4 is still in the preclinical development stage.

      • Properties
        • Alternative Name
          3,11-difluoro-6,8,13-trimethyl-8H-quinolino[4,3,2-kl]acridin-13-ium methyl sulfate
          CAS Number
          390362-78-4
          Molecular Formula
          C23H20F2N2O4S
          Molecular Weight
          458.48
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in EtOH; ≥10.54 mg/mL in DMSO; ≥2.51 mg/mL in H2O with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Chen H, Sun H, et al. "Monitoring autophagy in live cells with a fluorescent light-up probe for G-quadruplex structures." Chem Commun (Camb). 2019 Apr 25;55(35):5060-5063. PMID:30907894
          2. SugeZhang, HongxiaSun, et al. "Evaluation of the selectivity of G-quadruplex ligands in living cells with a small molecule fluorescent probe." Analytica Chimica Acta: X. Available online 23 April 2019, 100017.

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