nucleolar

Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2.

KI-CDK9d-32 is a CDK9 PROTAC degrader with a DC50 of 0.89 nM. It facilitates the ubiquitination and degradation of CDK9, inhibits the MYC pathway, and disrupts nucleolar homeostasis. KI-CDK9d-32 demonstrates anticancer activity.

BMH-22 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

BMH-23 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

BMH-9 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

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

Rudolfomycin is a class II anthracycline antitumor antibiotic that inhibit the synthesis of nucleolar RNA in intact tumor cells.

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.

WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 ( WDR5 ), with a K d of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity [1] .