hnRNPK-IN-1 是一种异质核糖核蛋白 K (hnRNPK) 结合配体，用 SPR 和 MST 测量的 Kd 值分别为 4.6 μM 和 2.6 μM。hnRNPK-IN-1 通过破坏 hnRNPK 和 c-myc 启动子的结合来抑制 c-myc 转录。hnRNPK-IN-1诱导 Hela 细胞凋亡 (apoptosis)，并具有很强的抗肿瘤活性。
货号:ajcx34032
CAS:2313528-04-8
分子式:C23H21N3O5
分子量：419.43
溶解度:DMSO : 5 mg/mL (11.92 mM; ultrasonic and warming and heat to 80°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.