| Identification | Back Directory | [Name]
2-Propen-1-one, 1-(4-methoxyphenyl)-3-[4-(4-morpholinyl)-6-nitro-2-quinolinyl]-, (2E)- | [CAS]
2313528-04-8 | [Synonyms]
hnRNPK-IN-1
2-Propen-1-one, 1-(4-methoxyphenyl)-3-[4-(4-morpholinyl)-6-nitro-2-quinolinyl]-, (2E)- | [Molecular Formula]
C23H21N3O5 | [MDL Number]
MFCD34179487 | [MOL File]
2313528-04-8.mol | [Molecular Weight]
419.43 |
| Chemical Properties | Back Directory | [Boiling point ]
673.6±55.0 °C(Predicted) | [density ]
1.325±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 5 mg/mL (11.92 mM; ultrasonic and warming and heat to 80°C) | [form ]
Solid | [pka]
3.81±0.61(Predicted) | [color ]
Brown to orange |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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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