SEC inhibitor KL-1

SEC inhibitor KL-1 (KL-1) is a peptide-like lead compound that is an effective selective SEC inhibitor. SEC inhibitor KL-1 promotes apoptosis and has anti-tumor activity. SEC inhibitor KL-1 doses dependently inhibits the AFF4-CCNT1 interaction, with a Ki value of 3.48 μM^[1][2]. IC50 & Target:SEC^[2] In Vitro: SEC inhibitor KL-1 (0-100μM, 24-72h) inhibits the growth of DIPG cells and increases apoptosis^[1].
SEC inhibitor KL-1 for H3 wild-type astrocytes, the h3g34v mutant glioma cells, and NHA cells with IC₅₀ are 18, 16 and 18μM, respectively^[1].
SEC inhibitor KL-1 disrupts SEC, leading to increase occupancy of Pol II near the promoter, which can delay Pol II mutants and slow down Pol II's elongation rate^[2].
SEC inhibitor KL-1 (5h) blocks the induction of heat shock-induced genes FOS, HSPD1, HSPE1, and EGR1 in HCT116 cells, impairing the heat shock response^[2]. In Vivo: SEC inhibitor KL-1 (50 mg/kg, administered intraperitoneally, once daily, 15 days) disrupts SEC, which can slow down tumor progression and improve survival rates in MDA231-LM2 tumor mice^[2].