hnRNPK-IN-1

hnRNPK-IN-1 is a specific ligand that binds to the heterogeneous nuclear ribonucleoprotein K (hnRNPK) with high affinity, as evidenced by dissociation constant (Kd) values of 4.6 μM and 2.6 μM determined using surface plasmon resonance (SPR) and microscale thermophoresis (MST), respectively. This binding disrupts the interaction between hnRNPK and the c-myc promoter, thereby inhibiting c-myc transcription. Furthermore, hnRNPK-IN-1 induces apoptosis in HeLa cells and exhibits significant anti-tumor activity.

SPR assay:4.6 μM (Kd), hnRNPK:2.6 μM (Kd), MST assay:2.6 μM (Kd)

Method: Human cervical cancer cells (HeLa), human lung adenocarcinoma cells (A549), human osteosarcoma epithelial cells (U2OS), human melanoma cells (A375), and human hepatocellular carcinoma cells (HuH7) were treated with hnRNPK-IN-1 at graded concentrations for 48 h. Cell growth inhibition was assessed using the MTT assay.
Result: hnRNPK-IN-1 dose-dependently inhibited the proliferation of various cancer cells, with IC50 values of 2.21, 3.04, 1.36, 3.59, and 2.94 μM against HeLa, A549, U2OS, A375, and HuH7 cells, respectively. The IC50 value against normal HEK293 cells was 34.72 μM, demonstrating selective antiproliferative activity [1].
Method: HeLa cells were treated with hnRNPK-IN-1 (1.25, 2.5 μM) for 24 h. Chromatin immunoprecipitation (ChIP) assay was used to detect the binding of hnRNP K to the c-myc promoter DNA.
Result: hnRNPK-IN-1 dose-dependently disrupted the binding of hnRNP K to the c-myc promoter DNA, with significantly reduced amounts of hnRNP K-bound DNA observed in both the 1.25 μM and 2.5 μM treatment groups [1].

Method: Nude mice bearing HeLa cell xenografts (dosing initiated when tumor volume reached approximately 100 mm³) were intraperitoneally administered hnRNPK-IN-1 at doses of 6.7 and 20.0 mg/kg once daily for three weeks. A vehicle control group and a cisplatin group (1.0 mg/kg) were also included. Tumor volume and body weight were measured every two days, and tumor weight was measured at the end of the study.
Result: hnRNPK-IN-1 at doses of 6.7 and 20.0 mg/kg achieved tumor inhibition rates of 54.1% and 69.3%, respectively. Tumor weights in the treatment groups were significantly lower than those in the vehicle control group (mean 459.7 mg and 307.4 mg vs. 1000.1 mg, respectively) [1].

DMSO: 4 mg/mL (9.54 mM), Sonication is recommended.