Description
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.
Product information
CAS Number: 2313528-04-8
Molecular Weight: 419.43
Formula: C23H21N3O5
Chemical Name: (2E)-1-(4-methoxyphenyl)-3-[4-(morpholin-4-yl)-6-nitroquinolin-2-yl]prop-2-en-1-one
Smiles: COC1=CC=C(C=C1)C(=O)/C=C/C1C=C(C2=CC(=CC=C2N=1)[N+]([O-])=O)N1CCOCC1
InChiKey: PFTIJUIEMIEMQH-RUDMXATFSA-N
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+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (11.92 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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