Molecular Formula | C23H22N4O3S2 |
Molar Mass | 466.58 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
Use | HA15 is a highly effective and specific inhibitor of endoplasmic reticulum chaperone protein BiP/GRP78/HSPA5, which can inhibit the ATPase activity of BiP and has anti-tumor activity. |
In vitro study | HA15 induces endoplasmic reticulum stress in cells in vitro, leading to cancer cell death; In melanoma cells, it overcomes resistance to BRAF inhibitors. |
In vivo study | In a xenograft mouse model (harboring melanoma cells that are sensitive or resistant to BRAF inhibitors),HA15 is able to induce endoplasmic reticulum stress leading to cancer cell death. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.143 ml | 10.716 ml | 21.433 ml |
5 mM | 0.429 ml | 2.143 ml | 4.287 ml |
10 mM | 0.214 ml | 1.072 ml | 2.143 ml |
5 mM | 0.043 ml | 0.214 ml | 0.429 ml |
biological activity | HA15 is a small molecule that specifically targets HSPA5 (Heat shock 70kDa protein 5), which can also be called BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). It has anti-tumor activity in the detected melanoma cells, including cells isolated from patients and cells resistant to BRAF inhibitors. |
target | TargetValue BiP/GRP78/HSPA5 () |
Target | Value |
in vitro study | HA15 induces endoplasmic reticulum stress in in vitro cells, leading to cancer cell death; in melanoma cells, overcome its resistance to BRAF inhibitors. |
In vivo studies | In a xenograft mouse model (carrying melanoma cells that are sensitive or resistant to BRAF inhibitors),HA15 can induce endoplasmic reticulum stress, which leads to cancer cell death. |