pol-1-in-1

Pol I-IN-1 is a potent inhibitor of RNA polymerase I (Pol I), specifically targeting the large catalytic subunit RPA194, with an inhibition concentration (IC50) of 0.21 μM [1].

POL1-IN-1 (Compound 3A) can effectively inhibit the transcription of RNA polymerase I in the A375 malignant melanoma cell line but has no effect on polymerase II.

RNA polymerase II-IN-2 (compound 20iii), a potent inhibitor of RNA polymerase II (Pol II) with a K i value of 9.5 nM, exhibits cytotoxicity against cancer cells, demonstrating toxicity levels 2 and 5 times higher than α-amanitin in CHO and HEK293 cells, respectively [1].

Pol (476-484), HIV-1 RT Epitope, is a biologically active peptide representing the dominant HLA A*0201-restricted epitope within HIV-1 reverse transcriptase (RT). Spanning Pol residues 476-484, it is utilized to explore mechanisms of HIV-1 escape from cytotoxic T lymphocytes (CTL) with IV9 as the specific epitope processed and presented in HIV-1-infected cell lines.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

RNA polymerase II-IN-1 (compound 19iv), an amatoxin, selectively inhibits RNA polymerase II (Pol II) with an IC50 of 36.66 nM and exhibits heightened cytotoxicity towards cancer cells while reducing toxicity in normal cells compared to α-Amanitin [1].