| 应用 |
A highly potent HSP90 inhibitor to HSP90α and HSP90β |
| 产品介绍 |
Luminespib (AUY-922, NVP-AUY922)是一种高效的HSP90抑制剂，其对HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何HSP90配体均可紧密结合。Phase 2。 |
| 备注 |
AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2. |
| 生化机理 |
NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of Hsp90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to Hsp90. NVP-AUY922 causes p23 dissociation from the Hsp90 complex and can then recruit HSP70 to the Hsp90 complex. Meanwhile, treatment with NVP-AUY922 causes decreased expression of HER-2 in NCI-N87 cells. NVP-AUY922 treatment results in binding of Hsp90 to client proteins and setting them up as targets for degradation by the proteasome.NVP-AUY922 can influence cell growth by affecting mutiple signaling pathways. |
| 别名 |
5-[2,4-二羟基-5-异丙基苯基]-N-乙基-4-[4-(4-吗啉基甲基)苯基]-3-异恶唑甲酰胺;AUY922;VER-52296;NVP-AUY 922;AUY-922;VER 52296;VER52296;5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide |
