1. Apoptosis
  2. c-Myc Apoptosis
  3. hnRNPK-IN-1

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.

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hnRNPK-IN-1 Chemical Structure

hnRNPK-IN-1 Chemical Structure

CAS No. : 2313528-04-8

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Based on 1 publication(s) in Google Scholar

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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[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].

MedChemExpress (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].

MedChemExpress (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.
Molecular Weight

419.43

Formula

C23H21N3O5

CAS No.
Appearance

Solid

Color

Brown to orange

SMILES

O=C(C1=CC=C(OC)C=C1)/C=C/C2=NC3=CC=C([N+]([O-])=O)C=C3C(N4CCOCC4)=C2

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
In Vitro: 

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)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3842 mL 11.9209 mL 23.8419 mL 59.6047 mL
5 mM 0.4768 mL 2.3842 mL 4.7684 mL 11.9209 mL
10 mM 0.2384 mL 1.1921 mL 2.3842 mL 5.9605 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
hnRNPK-IN-1
Cat. No.:
HY-135691
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