HMN214

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HMN-214(IVX214) 是一种有效的 PLK1 抑制剂，平均 IC50 为 0.12 μM。

HMN-214 is an oral prodrug of HMN-176, a stilbene derivative that interferes with the subcellular spatial location of polo-like kinase-1, a serine/threonine kinase that regulates critical mitotic events.(In Vitro):HMN-214 is a prodrug of HMN-176. HMN-176 shows potent activities against 22 human tumor cell lines, with a mean IC50s of 118 nM. HMN-176 (3-300 nM) inhibits luciferase expression driven by the MDR1 promoter in a dose dependent manner in HeLa cells. HMN-176 (30-3000 nM) also dose-dependently suppresses complex formation on the Y-box. HMN-214 (3.3 μM) enhances luciferase expression relative to vehicle control with the 1,4C-1,4Bis polymer (11-fold) and PEI (37-fold) in PC3-PSMA cells. HMN-214 (≥ 3.3 μM) significantly reduces cell proliferation, causes considerable changes in cell morphology in MB49 cells.(In Vivo):HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. HMN-214 has no effect on the conduction velocity and the amplitude of action potentials in the aciatic and tibial nerves. HMN-214 (20 mg/kg, p.o.) exhibits antitumor activity in mice. HMN-214 (10, 20 mg/kg, p.o.) decreases MDR1 mRNA expression in nude mice bearing KB- and KB-A.1.-derived tumors.

HMN-214 is a prodrug of HMN-176. HMN-176 shows potent activities against 22 human tumor cell lines, with a mean IC50s of 118 nM. HMN-176 (3-300 nM) inhibits luciferase expression driven by the MDR1 promoter in a dose dependent manner in HeLa cells. HMN-176 (30-3000 nM) also dose-dependently suppresses complex formation on the Y-box. HMN-214 (3.3 μM) enhances luciferase expression relative to vehicle control with the 1,4C-1,4Bis polymer (11-fold) and PEI (37-fold) in PC3-PSMA cells. HMN-214 (≥ 3.3 μM) significantly reduces cell proliferation, causes considerable changes in cell morphology in MB49 cells.

HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. HMN-214 has no effect on the conduction velocity and the amplitude of action potentials in the aciatic and tibial nerves. HMN-214 (20 mg/kg, p.o.) exhibits antitumor activity in mice. HMN-214 (10, 20 mg/kg, p.o.) decreases MDR1 mRNA expression in nude mice bearing KB- and KB-A.1.-derived tumors.

HMN214 | HMN 214 | HMN-214

Microbiology/Virology

HIV

PLK1

Cancer

——

173529-46-9

424.47

C22H20N2O5S

>98% (HPLC)

DMSO : 25 mg/mL 58.90 mM;

CC(=O)N(c1ccccc1/C=C/c1cc[n+](cc1)[O-])S(=O)(=O)c1ccc(cc1)OC

(E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide

(-20℃)

With Ice Pack

≥ 2 years