hnRNPK-IN-1

• CAT Number: I044515
• CAS Number: 2313528-04-8
• Molecular Formula: C23H21N3O5
• Molecular Weight: 419.43
• Purity: ≥95%
• Synonyms: (E)-1-(4-methoxyphenyl)-3-(4-morpholin-4-yl-6-nitroquinolin-2-yl)prop-2-en-1-one
• InChI: InChI=1S/C23H21N3O5/c1-30-19-6-2-16(3-7-19)23(27)9-4-17-14-22(25-10-12-31-13-11-25)20-15-18(26(28)29)5-8-21(20)24-17/h2-9,14-15H,10-13H2,1H3/b9-4+
• InChIKey: PFTIJUIEMIEMQH-RUDMXATFSA-N
• SMILES: COC1=CC=C(C=C1)C(=O)C=CC2=CC(=C3C=C(C=CC3=N2)[N+](=O)[O-])N4CCOCC4

hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd 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[1].
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[1].?
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[1].?
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[1].?
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[1].
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[1].

Reference

[1]. Bing Shu, et al. Syntheses and evaluation of new Quinoline derivatives for inhibition of hnRNP K in regulating oncogene c-myc transcription. Bioorg Chem. 2019 Apr;85:1-17.
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