All AbMole products are for research use only, cannot be used for human consumption.
HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G(2)/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1α and VEGF which play an important role in angiogenesis. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Combined treatment of Sorafenib and HS-173 synergistically inhibited the viability of Panc-1 cells (combination index<1). HS-173 demonstrated anti-proliferative effects in NSCLC cells and effectively inhibited the PI3K signaling pathway in a dose‑dependent manner.HS-173 reduced the expression of α-smooth muscle actin (α-SMA), vimentin, PAI-1, fibronectin, collagen type I, collagen IV and TGF-β-activated smad2/3 in PD-derived primary fibroblasts.
 |
Source | Oncotarget (2016). Figure 2. HS-173 |
| Method | wound healing assay | |
| Cell Lines | Miapaca-2 and Aspc-1 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | In three pancreatic cancer cell lines, TGF-β treated group was healed over 90% of the wound area within 16 h, whereas cells in control group were slowly migrated. However, HS-173 successfully suppressed TGF-β induced cell migration dose-dependently in all pancreatic cancer cell lines |
| Cell Experiment | |
|---|---|
| Cell lines | T47D, SK-BR3, MCF7 cells |
| Preparation method | Using a MTT assay to performe cell viability . Briefly, plating T47D cells in 96-well plates for 24 h. Then,removing the medium and treating cells with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After incubating the cells for 48 h, adding 20 μL MTT solution (5 mg/mL) to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. Then read the plate on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose−response curves. To assess the effect of compounds on cell proliferation, culturing T47D cells with compound (0.1−100 μM) for 48 h before MTT analysis. |
| Concentrations | ~50 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Male BALB/c mice with CCl4-induced liver fibrosis |
| Formulation | Dissolved in DMSO, and then mixture (DMSO:PEG400:D.W. = 1:5:4). |
| Dosages | ~20 mg/kg |
| Administration | p.o. |
| Molecular Weight | 422.46 |
| Formula | C21H18N4O4S |
| CAS Number | 1276110-06-5 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
