中文同义词:
6-氨基-8-[(3,5-二氯苯基)硫基]-N-异丙基-9H-嘌呤-9-丙胺;HSP90抑制剂(PU-WS13)
英文同义词:
PU-WS13;8-((3,5-dichlorophenyl)thio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine;6-Amino-8-[(3,5-dichlorophenyl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine;8-(3,5-dichlorophenyl)sulfanyl-9-[3-(propan-2-ylamino)propyl]purin-6-amine;PU WS13;PUWS13;CS-1689;CS-2047;9H-Purine-9-propanamine, 6-amino-8-[(3,5-dichlorophenyl)thio]-N-(1-methylethyl)-
沸点
617.4±65.0 °C(Predicted)
密度
1.47±0.1 g/cm3(Predicted)
储存条件
Keep in dark place,Sealed in dry,2-8°C
酸度系数(pKa)
10.15±0.29(Predicted)
生物活性
PU-WS13 是一种选择性的 Grp94 抑制剂,EC50 值为 0.22 μM。
靶点
GRP94
0.22 μM (EC 50 )
HSP90α
27.3 μM (EC 50 )
HSP90β
41.8 μM (EC 50 )
TRAP-1
7.3 μM (EC 50 )
GRP94
0.22 μM (EC 50 )
HSP90α
27.3 μM (EC 50 )
体外研究
PU-WS13 is a Grp94 inhibitor, with an EC 50 of 0.22 μM. PU-WS13 also slightly suppresses Hsp90α, Hsp90β and Trap-1, with EC 50 s of 27.3, 41.8 and 7.3 μM, respectively. PU-WS13 (2.5-20 μM) shows no toxicity on two nonmalignant cell lines. PU-WS13 (15 μM) disrupts the circular architecture of HER2 at the plasma membrane of SKBr3 cells mediated through Grp94. PU-WS13 inhibits Grp94, and the inhibition induces apoptosis in and reduce the viability of HER2 overexpressing breast cancer cells.