CAY10698 (compound 1) 是一种有效的选择性 12-Lipoxygenase (12-LOX) 抑制剂,IC50 为 5.1 μM。
Cas No. |
684236-01-9 |
Canonical SMILES |
COC1=C(O)C(CNC2=CC=C(S(NC3=NC=CS3)(=O)=O)C=C2)=CC=C1 |
分子式 |
C17H17N3O4S2 |
分子量 |
391.5 |
溶解度 |
DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 20 mg/ml,Ethanol: 0.5 mg/ml |
储存条件 |
4°C, protect from light |
General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition |
Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
半岛bd体育手机客户端 描述 |
Platelet-type 12-lipoxygenase catalyzes the formation of 12-HpETE from arachidonic acid . It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines. It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function. CAY10698 is an inhibitor of 12-LO with an IC50 value of 5.1 ?M. It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = >50, >40, and >200 ?M. The scaffold of this compound has been subjected to medicinal chemistry optimization and biological characterization for development of potential 12-LO inhibitors. |