Supplier of assay kits antibodies biochemicals and proteins and provider of contract research services. Cx 5461 is a first in class non genotoxic small molecule targeted inhibitor of rna polymerase i pol i that activates the p53 pathway without causing dna damage.
Cx 5461 Senhwa Biosciences Inc
Abstract Introduction
Cx 5461
Cx 5461 exhibits antiproliferative activity against human pancreatic t.
Cx 5461 structure. Please enable javascript to view this page. Cx 5461 is an inhibitor of rrna synthesis selectively inhibits pol i driven transcription of rrna with ic50 of 142 nm has no effect on pol ii and possesses 250 to 300 fold selectivity for inhibiti on of rrna transcription versus dna replication and protein translation. Cx 5461 selectively inhibits rrna synthesis by pol i in the nucleolus but does not inhibit mrna synthesis by rna polymerase ii pol ii and does not inhibit dna replication or protein synthesis.
The median ec50 across all tested cell lines is 147 nm yet all normal cell lines have ec50 values of approximately 5 000 nm. Cx 5461 is a first in class non genotoxic small molecule targeted inhibitor of rna polymerase i pol i that activates the p53 pathway without causing dna damage. Cx 5461 is a potent and oral rrna synthesis inhibitor.
In contrast bmh 21 revealed no detectable g4 binding or stabilization fig. A chemical formula is a way of expressing information about the proportions of atoms that constitute a particular chemical compound using a single line of chemical element symbols and numbers. Pubchem uses the hill system whereby the number of carbon atoms in a molecule is indicated first the number of hydrogen atoms second.
Cx 5461 is a potent and orally bioavailable small molecule inhibitor of rrna synthesis that specifically inhibits rna polymerase pol i driven transcription with ic50 value of 142 nm. To assess the ability of stabilized g4 sequences to stall a dna polymerase we performed an in vitro dna polymerase extensionprocessivity assay 30. Cx 5461 induced significant growth inhibition in wild type wt and mutant tp53 myeloma cell lines and primary samples in association with increases in downstream markers of apoptosis.
Cx 5461 exhibits broad antiproliferative potency in a panel of cancer cell lines in human cancer cell lines but has minimal effect on viability of nontransformed human cells. It inhibits rna polymerase i driven transcription of rrna with ic50s of 142 113 and 54 nm in hct 116 a375 and mia paca 2 cells respectively. Strikingly same as pds.
Moreover pol i inhibition overcame adhesion mediated drug resistance and resistance to conventional and novel agents. Cx 5461 is a g quadruplex stabilizer in the human genome.
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Selective Inhibition Of Rna Polymerase I Transcription As A
Small Molecule Targeting Of Rna Polymerase I Activates A Conserved
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