PP 2 (AG 1879) is a selective Src family kinase inhibitor[1]. The IC50 values of PP 2 for inhibiting Lck and Fyn are 0.004μM and 0.005μM, respectively[2].
In vitro, PP 2 (10μM; 30min) inhibits PrP106-126-induced iNOS activation mediated by CD36 in BV2 microglia[3]. PP 2 (5, 10 or 20μM; 24, 48 or 72 h) suppresses growth and induces apoptosis in HNSCC cell lines[4].
In vivo, PP 2 (2mg/kg; 8 weeks; i.p.) ameliorates renal fibrosis by regulating the NF-κB/COX-2 and PPAR γ/UCP2 pathway in diabetic mice[1]. PP 2 (1mg/kg; 4 days; i.p.) protects from keratin mutation–associated liver injury and filament disruption via SRC kinase inhibition in male mice[5].
References:
[1] Wei J, Deng X, Li Y, et al. PP2 Ameliorates Renal Fibrosis by Regulating the NF-κB/COX-2 and PPARγ/UCP2 Pathway in Diabetic Mice. Oxid Med Cell Longev. 2021 Sep 17;2021:7394344.
[2] Hanke JH, Gardner JP, Dow RL, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[3] Zhang S, Yang L, Kouadir M, et al. PP2 and piceatannol inhibit PrP106-126-induced iNOS activation mediated by CD36 in BV2 microglia. Acta Biochim Biophys Sin (Shanghai). 2013 Sep;45(9):763-72.
[4] Lee S, Park S, Ryu JS, et al. c-Src inhibitor PP2 inhibits head and neck cancer progression through regulation of the epithelial-mesenchymal transition. Exp Biol Med (Maywood). 2023 Mar;248(6):492-500.
[5] Li P, Maitra D, Kuo N, et al. PP2 protects from keratin mutation-associated liver injury and filament disruption via SRC kinase inhibition in male but not female mice. Hepatology. 2023 Jan 1;77(1):144-158.
PP 2 (AG 1879)是一种选择性Src家族激酶抑制剂[1]。PP 2抑制Lck和Fyn的半数抑制浓度（IC50）分别为0.004μM和0.005μM[2]。
在体外实验中，PP 2（10μM; 30分钟）可抑制PrP106-126诱导的、通过CD36介导的BV2小胶质细胞中iNOS的激活[3]。PP 2（5, 10或20μM; 24, 48或72小时）可抑制头颈部鳞状细胞癌（HNSCC）细胞系的生长，并诱导其凋亡[4]。
在体内实验中，PP 2（2mg/kg; 8周; 腹腔注射）通过调节NF-κB/COX-2和PPARγ/UCP2通路，在糖尿病小鼠中可改善肾纤维化[1]。PP 2（1mg/kg; 4天; 腹腔注射）通过抑制Src激酶，在雄性小鼠中可保护机体免受角蛋白突变相关的肝脏损伤和丝状结构破坏[5]。