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PF-00562271 Besylate
PF-00562271 Besylate (PF-562271) 是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。Phase 1。
PF-562271
PF-562271 (PF-00562271)是一种有效的，ATP竞争性的，可逆的FAK抑制剂，无细胞试验中IC50为1.5 nM，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N 4, SEM, *p 0.05 vs respective control (D and E).
PRT062607 (P505-15) HCl
PRT062607 (P505-15, BIIB057, PRT-2607)是一种新型的，高度选择性Syk抑制剂，无细胞试验中IC50为1 nM，作用于Syk比作用于Fgr，PAK5，Lyn，FAK，Pyk2, FLT3, MLK1 和Zap70选择性高80倍以上。
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
PF-573228
PF-573228 是一种ATP竞争性的FAK抑制剂，无细胞试验中IC50为4 nM，作用于FAK比作用于Pyk2，CDK1/7 和 GSK-3β选择性高~50到250倍。PF-573228 可诱导凋亡。
OVISE cells were incubated for 25 hr at the indicated concentrations of the FAK inhibitors. Immunoblots were performed to assess inhibition of auto-phosphorylation by the FAK inhibitors.
TAE226 (NVP-TAE226)
TAE226 (NVP-TAE226) 是一种有效的FAK抑制剂，IC50为5.5 nM，最有效作用于Pyk2，对InsR， IGF-1R， ALK和c-Met作用效果比其弱10到100倍左右。TAE226 (NVP-TAE226) 可诱导凋亡。
Targeting the actin cytoskeleton overcomes resistance to HDACi in primary MM. Graphs representing the proportion of cell death induced in MM patients (n=6) treated LBH589 (5 nM), TAE226 (0.5 uM) and combination.
PF-562271 HCl
PF-562271 HCl是PF-562271的盐酸盐形式，是一种强效的ATP竞争性的可逆的抑制剂，作用于FAK其IC50为1.5 nM。相比较FAK，对Pyk2的效果少了大约十倍，除了CDKs类的蛋白酶，PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N 4, SEM, *p 0.05 vs respective control (D and E).
BI-4464
BI-4464是高选择性、ATP竞争性的PTK2/FAK抑制剂，IC50为17 nM。
Y15
Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
GSK2256098
GSK2256098 是一种有效的、选择性的、可逆的、ATP竞争性的 FAK kinase 抑制剂，apparent Ki为0.4 nM。GSK2256098 可抑制癌细胞生长并诱导凋亡。
PND-1186 (VS-4718)
PND-1186 (VS-4718, SR-2156) 是一种可逆的选择性FAK抑制剂，IC50为1.5 nM。PND-1186 可选择性地促进肿瘤细胞的凋亡。Phase 1。
(a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 M or 1 M PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean SD (*P 0.05; **P 0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 M or 1 M PND 1186. -tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 M or 1 M PND 1186 (*P 0.05; **P 0.01; versus Vehicle, n =3).
Defactinib (VS-6063)
Defactinib (VS-6063, PF-04554878)是一种选择性，且口服有效的FAK抑制剂。Phase 2。
Immunofluorescence microscopy (1000x magnification) with p65 (red fluorescence, Cy3) revealed a cytoplasmic retention of p65 after VS-6063 treatment in HBl-2 and MINO (D).
Solanesol (Nonaisoprenol)
Solanesol (Nonaisoprenol, Betulanonaprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants.
PF-00562271 Besylate (PF-562271) 是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。Phase 1。
PF-562271 (PF-00562271)是一种有效的，ATP竞争性的，可逆的FAK抑制剂，无细胞试验中IC50为1.5 nM，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N 4, SEM, *p 0.05 vs respective control (D and E).
PRT062607 (P505-15) HCl
PRT062607 (P505-15, BIIB057, PRT-2607)是一种新型的，高度选择性Syk抑制剂，无细胞试验中IC50为1 nM，作用于Syk比作用于Fgr，PAK5，Lyn，FAK，Pyk2, FLT3, MLK1 和Zap70选择性高80倍以上。
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
PF-573228 是一种ATP竞争性的FAK抑制剂，无细胞试验中IC50为4 nM，作用于FAK比作用于Pyk2，CDK1/7 和 GSK-3β选择性高~50到250倍。PF-573228 可诱导凋亡。
OVISE cells were incubated for 25 hr at the indicated concentrations of the FAK inhibitors. Immunoblots were performed to assess inhibition of auto-phosphorylation by the FAK inhibitors.
TAE226 (NVP-TAE226) 是一种有效的FAK抑制剂，IC50为5.5 nM，最有效作用于Pyk2，对InsR， IGF-1R， ALK和c-Met作用效果比其弱10到100倍左右。TAE226 (NVP-TAE226) 可诱导凋亡。
Targeting the actin cytoskeleton overcomes resistance to HDACi in primary MM. Graphs representing the proportion of cell death induced in MM patients (n=6) treated LBH589 (5 nM), TAE226 (0.5 uM) and combination.
PF-562271 HCl是PF-562271的盐酸盐形式，是一种强效的ATP竞争性的可逆的抑制剂，作用于FAK其IC50为1.5 nM。相比较FAK，对Pyk2的效果少了大约十倍，除了CDKs类的蛋白酶，PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。
VEGF and P450 enzyme production in response to FAK or Src inhibitors. MCF10A cells were cultured in LD collagen gels ?vehicle control (V), 10 uM PF-562271 FAK ATP inhibitor (PF) or Src inhibitor PP2 for 24 h. Cells were also lysed and examined for CYP1A1 or CYP4B1 by immunoblot (B and C) and densitometry (D and E). VEGF data are displayed as the mean normalized to the vehicle control, N = 6, 盨EM, *p 0.003 vs control (A). P450 data are displayed as the mean relative to GAPDH and normalized to the control. N 4, SEM, *p 0.05 vs respective control (D and E).
Y15 (1,2,4,5-Benzenetetraamine tetrahydrochloride, FAK inhibitor 14) is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
GSK2256098 是一种有效的、选择性的、可逆的、ATP竞争性的 FAK kinase 抑制剂，apparent Ki为0.4 nM。GSK2256098 可抑制癌细胞生长并诱导凋亡。
PND-1186 (VS-4718)
PND-1186 (VS-4718, SR-2156) 是一种可逆的选择性FAK抑制剂，IC50为1.5 nM。PND-1186 可选择性地促进肿瘤细胞的凋亡。Phase 1。
(a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 M or 1 M PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean SD (*P 0.05; **P 0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 M or 1 M PND 1186. -tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 M or 1 M PND 1186 (*P 0.05; **P 0.01; versus Vehicle, n =3).
Defactinib (VS-6063, PF-04554878)是一种选择性，且口服有效的FAK抑制剂。Phase 2。
Immunofluorescence microscopy (1000x magnification) with p65 (red fluorescence, Cy3) revealed a cytoplasmic retention of p65 after VS-6063 treatment in HBl-2 and MINO (D).
Solanesol (Nonaisoprenol)
Solanesol (Nonaisoprenol, Betulanonaprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants.
Tags: FAK activation | FAK signaling | FAK cancer | FAK phosphorylation | Focal Adhesion Kinase cancer | Focal Adhesion Kinase signaling | FAK inhibition | Focal Adhesion Kinase activation | Focal Adhesion Kinase phosphorylation | FAK assay | FAK inhibitor clinical trial | FAK cleavage | FAK inhibitor review
