Oncrasin-1

Oncrasin-1 is an RNA polymerase inhibitor. Oncrasin-1 suppresses the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells. Oncrasin-1 effectively kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 leads to coaggregation of PKCι and splicing factors into megaspliceosomes. Oncrasin-1 induces malfunction in the RNA processing machinery. Oncrasin-1 is an anti-cancer agent and can therefore be studied in research for lung cancer^[1][2]. In Vitro:Oncrasin-1 (0.1-33 μM, 3 d) induces dose-dependent cytotoxicity in T29Kt1 cells (IC₅₀ = 4.81 μM)^[1].
Oncrasin-1 (31 nM-33 μM) effectively kills K-Ras-mutant H460, H2122, H2887, and A549 cells with an IC₅₀ ≤ 3 μM^[1].
Oncrasin-1 (1-10 μM, 12 h) increases the apoptotic cell percentages and leads to a substantial change in the subcellular localization of PKCι in both H460 and T29K1 cells^[1].
Oncrasin-1 (33 nM-3.3 μM, 24 h) shows its cytotoxic effect in cancer cells (H460) is due to its induction of apoptosis in H460 cells^[1].
Oncrasin-1 (1 μM, 12 h) shows that K-Ras is required to induce apoptosis^[1].
Oncrasin-1 (1 μM, 4-12 h) markedly inhibits expression of luciferase in H460 and T27Kt1 cells but has no effect of only mild effect in T29 cells^[2].
Oncrasin-1 (1 μM, 12 h) disrupts the interaction between PKCι and cyclin T1 and leads to transcription dysfunction in H460 cells^[2]. In Vivo:Oncrasin-1 (100 mg/kg, i.p., daily for 10 days) suppresses tumor growth by 75.4% and leads to prolonged survival in nude mice inoculated with H460 cells into the dorsal flank^[1].