MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂,具有中枢神经系统活性,IC50为 0.76 nM,有潜力用于帕金森氏病。
产品描述
MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).
体外活性
MLi-2, a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity.?MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).?MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels.
体内活性
MLi-2, a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity.?MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).?MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels.
Cas No.
1627091-47-7
分子式
C21H25N5O2
分子量
379.46
储存和溶解度
DMSO:60 mg/mL (158.12 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years