[CAS NO. 2313528-04-8] hnRNPK-IN-1
PRODUCTS SPECIFICATIONS [2313528-04-8]
DESCRIPTION [2313528-04-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 419.43 |
| Molecular Formula | C23H21N3O5 |
| SMILES | O=C(C1=CC=C(OC)C=C1)/C=C/C2=NC3=CC=C([N+]([O-])=O)C=C3C(N4CCOCC4)=C2 |
Summary
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 [1] .
IC50 & Target
Kd: 4.6 μM (hnRNPK; SPR assay) and 2.6 μM (hnRNPK; MST assay) [1]
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
[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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell 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-PCR [1]
| Cell 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 Analysis [1]
| Cell 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 [1] .
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 [1] |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5 mg/mL ( 11.92 mM ; ultrasonic and warming and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3842 mL | 11.9209 mL | 23.8419 mL |
| 5 mM | 0.4768 mL | 2.3842 mL | 4.7684 mL |
| 10 mM | 0.2384 mL | 1.1921 mL | 2.3842 mL |