纯度:>98% by HPLC;NMR (Conforms)
分子式:C21H24F3N7O2
分子量:463.47
溶剂:DMSO (>25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):WNK kinase inhibitor
Function / Pharmacology:Potent and selective pan-With-No-Lysine (WNK) kinase inhibitor (IC50’s: WNK1 = 5 nM, WNK2 = 1 nM, WNK3 = 6 nM, WNK4 = 9 nM), an important enzyme in blood pressure regulation and body fluid and electrolyte homeostasis.1 WNK kinases respond to hypertonicity by regulating SLC12 cation chloride transporters to rescue cell volume.2 WNK463 reduced migration of invasive types of breast cancer and attenuated tumor growth and metastatic burden in a mouse model.3 It induced a significant increase in NLRP3 inflammasome activation and pyroptosis specifically via WNK1 inhibition as well as increasing TNF production without inflammasome activation.4