HS-173

SKU: orb1305733

Description

HS-173 is a potent and selective small molecule inhibitor of PI3Kα, exhibiting an IC50 of 0.8 nM. It is a valuable research tool for studying the PI3K/AKT signaling pathway in cancer biology, applicable in both in vitro cellular assays and in vivo xenograft models for oncology research.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1276110-06-5
• MW: 422.46
• Purity: 99.64%
• Formula: C₂₁H₁₈N₄O₄S
• SMILES: CCOC(=O)c1cnc2ccc(cn12)-c1cncc(NS(=O)(=O)c2ccccc2)c1
• Target: PI3K,Apoptosis
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:78 mg/mL (184.63 mM)

Bioactivity

• Target IC50:
  PI3Kα:0.8 nM
• In Vivo:
  In vitro studies reveal that HS-173 can induce apoptosis by affecting cell cycle distribution and activating caspases, while also inhibiting VEGF-induced angiogenesis. When combined with sorafenib, HS-173 exhibits synergistic anticancer effects in pancreatic cancer cells. Additionally, HS-173 demonstrates significant anti-proliferative activity in T47D, SK-BR3, and MCF7 cells (IC50: 0.6/1.5/7.8 μM), and fully inhibits the PI3K pathway in cancer cell lines (Hep3B and SkBr3).
• In Vitro:
  By inhibiting the PI3K/Akt signaling pathway, HS-173 significantly slows down the progression of liver fibrosis in vivo. It also reduces angiogenesis in mice.
• Cell Research:
  Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated 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 the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added 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. The plate is then read 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, T47D cells are cultured with compound (0.1 100 μM) for 48 h before MTT analysis.(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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Inhibitor, HS 173, HS173, HS-173, inhibit, PI3Kα, PI3K, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

52936849