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- Taro Mannena, .et al. Distinct RNA polymerase transcripts direct the assembly of phase-separated DBC1 nuclear bodies in different cell lines, Mol Biol Cell, 2021, 32:ar33, 1-11 PMID: 34495685
- Shuichiro Okamoto, .et al. The rRNA synthesis inhibitor CX-5461 may induce autophagy that inhibits anticancer drug-induced cell damage to leukemia cells, Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
- Ahmed Abdullah Ahmed, .et al. A G-quadruplex-binding compound shows potent activity in human gemcitabine-resistant pancreatic cancer cells, Sci Rep, 2020, 10: 12192 PMID: 32699225
- Abed Saady, .et al. Applying styryl quinolinium fluorescent probes for imaging of ribosomal RNA in living cells, Dyes Pigm, 2020, 174: 107986
- Jackobel AJ, .et al. DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism, Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
- Hiroaki Suzuki, .et al. The proline-arginine repeat protein linked to C9-ALS/FTD causes neuronal toxicity by inhibiting the DEAD-box RNA helicase-mediated ribosome biogenesi, Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
- Anastasia Gelgor, .et al. Nucleolar stress enhances lytic reactivation of the Kaposi??s sarcoma-associated herpesvirus, Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
- Wang ZF, .et al. The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules, Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
- Yuko Fujiwara, .et al. A Nucleolar Stress-Specific p53-miR-101 Molecular Circuit Functions as an Intrinsic Tumor-Suppressor Network, EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
- Maïmouna Coura Kone, .et al. Three-Dimensional Distribution of UBF and Nopp140 in Relationship to Ribosomal DNA Transcription During Mouse Preimplantation Development, Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997
Biological Activity
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.
Targets
| A375 | MIA PaCa-2 | Pol I-driven transcription of rRNA (HCT-116, A375, MIA PaCa-2 cells) | HCT-116 | |
| 58 nM(ED50) | 74 nM(ED50) | 142 nM | 167 nM(ED50) |
| In vitro | DMSO | <1 mg/mL | |
| Water | Insoluble | ||
| Ethanol | DMF: Warmed: 3 mg/mL (5.84 mM) | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 19.47 mL | 97.35 mL | 194.7 mL |
| 0.5 mM | 3.89 mL | 19.47 mL | 38.94 mL |
| 1 mM | 1.95 mL | 9.74 mL | 19.47 mL |
| 5 mM | 0.39 mL | 1.95 mL | 3.89 mL |
*The above data is based on the productmolecular weight 513.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11065 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1138549-36-6 |
| Formula | C27H27N7O2S |
| M. Wt | 513.6 |
| Purity | >98% |
| Synonyms | CX5461 |
| SMILES | CC1=CN=C(C=N1)CNC(=O)C2=C3N(C4=CC=CC=C4S3)C5=C(C2=O)C=CC(=N5)N6CCCN(CC6)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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