FAK
FAK (focal adhesion kinase), also known as PTK2 protein tyrosine kinase 2 (PTK2), is a protein that, in humans, is encoded by the FAK gene. FAK is a focal adhesion-associated protein kinase involved in cellular adhesion and spreading processes. It has been shown that when FAK was blocked, breast cancer cells became less metastatic due to decreased mobility.
FAK is phosphorylated in response to integrin engagement, growth factor stimulation, and the action of mitogenic neuropeptides.Integrin receptors are heterodimeric transmembrane glycoproteins that cluster upon ECM engagement, leading to FAK phosphorylation and recruitment to focal adhesions.[13][14] FAK activity can also be attenuated by expression of its endogenous inhibitor known as FAK-related nonkinase (FRNK). Overexpression of FAK leads to inhibition of apoptosis and an increase in the prevalence of metastatic tumors.
-
PND-1186是高活性FAK抑制剂，IC50为1.5 nM。
More
-
PF-562271苯磺酸盐是可逆的ATP竞争性FAK抑制剂，IC50为1.5 nM，比对Pyk2和其它蛋白激酶的抑制性高10倍和100倍以上，但一些CDK除外。
More
-
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.
More
-
PND-1186是高活性FAK抑制剂，IC50为1.5 nM。
More
-
PF-562271苯磺酸盐是可逆的ATP竞争性FAK抑制剂，IC50为1.5 nM，比对Pyk2和其它蛋白激酶的抑制性高10倍和100倍以上，但一些CDK除外。
More
-
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.
More
