rrna synthesis

4-Thiouridine (4-SU) is a photoactivatable ribonucleoside analog that is widely used for RNA analysis, including short-range RNA-RNA crosslinking and nascent RNA labeling. The crosslinking thio moiety is attached directly to the nucleotide base, thus 4-SU

Erythromycin (E-Mycin) is a Macrolide and Macrolide Antimicrobial. The physiologic effect of erythromycin is by means of Decreased Sebaceous Gland Activity.

CX5461 is an rRNA synthesis inhibitor with oral activity that inhibits Pol I-driven rRNA transcription. CX5461 activates the DNA damage response and has antitumor activity in tumors such as ovarian cancer.

Clindamycin hydrochloride monohydrate (Clindamycin alcoholate) is a protein synthesis inhibitor used orally, capable of diminishing virulence factor expression in Staphylococcus aureus at sub-minimum inhibitory concentrations (sub-MICs). It acts by suppressing Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1), and alpha-haemolysin (Hla) production. Resistance to this compound emerges through enzymatic methylation at the antibiotic's 50S ribosomal subunit binding site (23S rRNA).

7-Methylguanosine 5'-diphosphate (7-Methyl-GDP) sodium, a cap analog, is utilized in the synthesis of mRNA cap analogues[1].

NusB-IN-1 (Compound 22r) is a highly effective, orally administered bacterial rRNA synthesis inhibitor with potent antimicrobial activity against MRSA and VRSA [1].

Amikacin disulfate (BAY-416651 sulfate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.

CX-5461 dihydrochloride is a potent, orally active inhibitor of Pol I-mediated rRNA synthesis that acts on HCT-116 cells (IC50: 142 nM), A375 cells (IC50: 113 nM) and MIA PaCa-2 cells (IC50: 54 nM), and to a lesser extent on Pol II (IC50 ≥ 25 μM).

Pidnarulex HCl is the salt form of CX-5461, 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 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. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species.