PHPS1 是Shp2的选择性抑制剂,对 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的Ki分别为 0.73,5.8,10.7,5.8 和 0.47 μM。
产品描述
PHPS1 is an inhibitor of Shp2. PHPS1 efficiently inhibits activation of Erk1/2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.
体外活性
PHPS1 (30 μM; 6 days) inhibits proliferation of human tumor cells[1]. PHPS1 (5-20 μM; 5-360 minutes) inhibits Erk1/2 but not Akt and Stat3 phosphorylation in a dose-dependent manner[1].
体内活性
PHPS1 (3 mg/kg; i.p. injection; every day during the last week on the high-fat diet) renders Ldlr-/- mice less susceptible to atherosclerosis development[2].
Cas No.
314291-83-3
分子式
C21H15N5O6S
分子量
465.44
别名
PHPS 1;PHPS-1
储存和溶解度
DMSO:16.25 mg/ml (34.91 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years