hnRNPK-IN-1

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. Form:Solid IC50& Target:Kd: 4.6 μM (hnRNPK,SPR assay) and 2.6 μM (hnRNPK,MST assay)

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet