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CX 5461
- Soluble in 0.1N HCl(aq)
- MF: C27H27N7O2S
- MW: 513.61
Description
CX 5461 is a selective inhibitor of RNA polymerase I transcription with a reported IC50 value of 0.88 µM and approximately 200-fold selectivity over RNA polymerase II. It inhibits rDNA transcription and activates p53-dependent apoptosis in susceptible tumor cells.
RNA polymerase I drives ribosomal RNA synthesis, a process frequently upregulated in rapidly proliferating cancer cells. CX 5461 is relevant for nucleolar stress research, ribosome biogenesis inhibition and hematologic tumor models.
Key Features
- Selective RNA polymerase I transcription inhibitor
- Suppresses rRNA/rDNA transcription
- Shows selectivity over RNA polymerase II
- Activates p53-dependent tumor cell apoptosis
Applications
- RNA Pol I transcription assays
- Nucleolar stress research
- Ribosome biogenesis studies
- Hematologic cancer model profiling
More Information
| Parent CAS No. | 1138549-36-6 |
|---|---|
| Chemical Name | 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-Benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide |
| SMILES | N12C3=CC=CC=C3SC1=C(C(NCC1=NC=C(C)N=C1)=O)C(=O)C1=C2N=C(N2CCCN(C)CC2)C=C1 |
| MFCD | MFCD21609261 |
| InChi | InChI=1S/C27H27N7O2S/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36) |
| InChiKey | XGPBJCHFROADCK-UHFFFAOYSA-N |
| CID | 25257557 |
| Short Description | RNAP1 inhibitor |
References
- M. Haddach et al. Discovery of CX-5461, the first direct and selective inhibitor of RNA Polymerase I, for cancer therapeutics. ACS Med. Chem. Lett. 2012, 3, 602-606.
- M.J. Bywater et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell 2012, 22, 51-65.
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