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RHPS4

Catalog No.
B6186
Telomerase inhibitor
Grouped product items
SizePriceStock Qty
10mg
$180.00
Ship with 10-15 days
50mg
$610.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: ~3 μM for M14 cells in 5-day growth inhibition assay

RHPS4 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.

Reference:
[1] Phatak P, Cookson JC,Dai F,Smith V,Gartenhaus RB,Stevens MF,Burger AM.  Telomere uncapping by the G-quadruplex ligand RHPS4 inhibits clonogenic tumour cell growth in vitro and in vivo consistent with a cancer stem cell targeting mechanism. Br J Cancer.2007 Apr 23;96(8):1223-33.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt458.48
Cas No.390362-78-4
FormulaC23H20F2N2O4S
SolubilitySoluble in DMSO
Chemical Name3,11-difluoro-6,8,13-trimethyl-8H-quinolino[4,3,2-kl]acridin-13-ium methyl sulfate
SDFDownload SDF
Canonical SMILESFC1=CC=C(N(C)C2=C3C4=[N+](C)C5=C(C=C(F)C=C5)C3=CC(C)=C2)C4=C1.COS(=O)([O-])=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

RHPS4

Related Biological Data

RHPS4

Related Biological Data

RHPS4