PTC-IN-1

PTC-IN-1 (IDB-002) (0.08-10 μM; 60 min) induces context-dependent translational elongation arrest in HCC-1143 cells, with a preference for aliphatic residues at position -1 of nascent polypeptide chains^[1].
PTC-IN-1 (0.3-30 μM) exhibits sequence-specific translational inhibitory activity in vitro, with its potency toward the aliphatic-rich tetramer motif reporter gene being up to 18-fold higher than that toward the acidic motif-rich reporter gene^[1].
PTC-IN-1 (50 μM; 30 min) binds to the PTC of human 80S ribosomes and forms sequence-specific spatial interactions with the aliphatic residues of the FPAK nascent polypeptide chain^[1].
PTC-IN-1 (0.001-100 μM; 15 min for HCC-1143, 15 min to 8 h for MCF7) activates ribotoxic stress responses in HCC-1143 and MCF7 cells via rapid and sustained JNK phosphorylation, a process associated with increased ribosome collisions^[1].

PTC-IN-1 (72 h) inhibits the proliferation of various MYC-dependent cancer cell lines with EC₅₀ values of 0.077, 0.14, 0.191, 0.295, and 0.456 μM against 22RV1, HCC-002, LS411N, MCF7, and MRC-5, respectively, and shows weak potency against normal MRC-5 fibroblasts^[1].