hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with K d values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities
In Vitro
hnRNPK-IN-1 (Compound 25; 1.25-5 μM; 24 hours) treatment induces Hela cells apoptosis could be due to its repression of cmyc transcription. hnRNPK-IN-1 (1.25-5 μM; 48 hours) treatment down-regulates c-myc gene transcription and expression in Hela cells in a dose-dependent manner. hnRNPK-IN-1 shows a selective anti-proliferative effect on human cancer cell lines (Siha, A549, Hela, U2OS, A375, HuH7 and HEK293 cells) with IC50 values ranged from 1.36 to 3.59 μM. hnRNPK-IN-1 could selectively bind to hnRNP K without significant interaction with c-myc promoter DNA. The binding of hnRNPK-IN-1 to hnRNP K could disrupt the interaction between hnRNP K and c-myc promoter DNA in vitro and in cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: Hela cells Concentration: 1.25 μM, 2.5 μM, 5 μM Incubation Time: 24 hours Result: Induced Hela cells apoptosis and apoptosis-related protein expressions. RT-PCRCell Line: Hela cells Concentration: 1.25 μM, 2.5 μM, 5 μM Incubation Time: 48 hours Result: Caused a reduction of c-myc mRNA in a dose-dependent manner in Hela cells. Western Blot AnalysisCell Line: Hela cells Concentration: 1.25 μM, 2.5 μM, 5 μM Incubation Time: 48 hours Result: The expression levels of c-MYC also decreased in a dose-dependent manner.
In Vivo
hnRNPK-IN-1 (Compound 25; 6.7-20 mg/kg; i.p.; once a day; for three weeks) exhibits good tumor growth inhibition in a Hela xenograft tumor model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c female nude mice (five weeks old) bearing Hela cells Dosage: 6.7 mg/kg, 20 mg/kg Administration: Intraperitoneal injection; once a day; for three weeks Result: Inhibited tumor growth in a Hela cervical xenograft.
