HMN-214

SKU: orb1305488

Description

HMN-214

Research Area

Cell Biology

Key Properties

• CAS Number: 173529-46-9
• MW: 424.47
• Purity: 99.28%
• Formula: C₂₂H₂₀N₂O₅S
• SMILES: N(S(=O)(=O)C1=CC=C(OC)C=C1)(C(C)=O)C2=C(/C=C/C=3C=CN(=O)=CC3)C=CC=C2
• Target: PLK
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.18 mM);DMSO:12 mg/mL (28.27 mM)

Bioactivity

• Target IC50:
  PLK1:0.12 μM.
• In Vivo:
  HMN-214 is an orally administered prodrug that quickly converts to HMN-176, with limited in vitro data available the active metabolite, HMN-176, demonstrates effective and broad-spectrum antitumor activity against a variety of cancer cell lines including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with an average IC50 value of 118 nM. HMN-176 at concentration ranging from 250 nM to 2.5 μM inhibits mitotic spindle assembly and at 2.5 μM also impedes microtubule formation fro the centrosome. These outcomes suggest that HMN-176's anticancer activity is, in part, mediated by disrupting centrosome-driven microtubule (MT) assembly during mitosis. Additionally, at 2.5 μM, HMN-176 delay the formation o the proper spindle assembly checkpoint in human RPE1 and CFPAC-1 cells. By disruptin the interaction betwee the NF-Y transcription factor an the MDR1 promoter, HMN-176 (3 μM) downregulate the expression o the multidrug resistance gene (MDR1). In HeLa cells, HMN-176 (3 μM) blocks cell cycle progression a the G2/M phase. HMN-176 also exhibits cytotoxic effects on both human and murine cell lines resistant to various treatments, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 Values ranging from 143 nM to 265 nM.
• In Vitro:
  HMN-214, an oral prodrug of HMN-176, exhibits superior oral bioavailability. In nude mouse models carrying multi-drug resistant KB-A. Cells, HMN-214 (10 mg/kg-20 mg/kg) significantly inhibit the expression of MDR1 mRNA. Additionally, in mouse xenograft models of PC-3, A549, and WiDr cells, HMN-214 (10 mg/kg-20 mg/kg) effectively suppresses tumor growth.
• Cell Research:
  Cells are seeded into a 96-well microplate at a density of 3 × 103–1 × 104 cells/well. Dilutions of HMN-214 or HMN-176 are adde the Next day an the plate is incubated for 72 hours the Inhibition of growth is measured b the MTT assay and IC50 Values are then obtained.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, HMN 214, HMN214, HMN-214, inhibit, IVX 214, IVX214, IVX-214, PLK, PLK1, Polo-like Kinase (PLK)

Quick Database Links

Gene Symbol

PLK