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Catalog No. Product Name Information Product Use Citations Product Validations
S2013 PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Cancer Commun (Lond), 2022, 42(3):205-222
J Biol Chem, 2022, 298(4):101748
Proc Natl Acad Sci U S A, 2021, 118(40)e2105367118
S2360 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.
S2672 PF-00562271 Besylate PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
Theranostics, 2022, 12(3):1097-1116
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3519
S2890 PF-562271 PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S5321 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.
Evid Based Complement Alternat Med, 2021, 2021:8810414
Oncotarget, 2016, 7(47):77683-77695
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
S7357 PF-562271 HCl PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
J Exp Clin Cancer Res, 2021, 40(1):364
Cancers (Basel), 2021, 13(24)6344
Nat Commun, 2020, 11(1):3282
S7653 PND-1186 (VS-4718) PND-1186 (VS-4718, SR-2156) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Int J Mol Sci, 2022, 23(2)833
J Exp Clin Cancer Res, 2021, 40(1):364
J Exp Clin Cancer Res, 2021, 40(1):91
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Theranostics, 2022, 12(3):1097-1116
Cell Death Dis, 2022, 13(1):54
Nat Commun, 2021, 12(1):3904
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Mol Cell, 2021, S1097-2765(21)00264-1
Sci Signal, 2021, 14(682)eabc1648
Biochem Pharmacol, 2021, S0006-2952(21)00185-4
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
Biomaterials, 2021, 279:121235
Int J Mol Sci, 2021, 22(2)E752
J Neurosci Methods, 2021, 356:109141
S2013 PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Cancer Commun (Lond), 2022, 42(3):205-222
J Biol Chem, 2022, 298(4):101748
Proc Natl Acad Sci U S A, 2021, 118(40)e2105367118
S2360 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.
S2672 PF-00562271 Besylate PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
Theranostics, 2022, 12(3):1097-1116
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3519
S2890 PF-562271 PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S5321 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.
Evid Based Complement Alternat Med, 2021, 2021:8810414
Oncotarget, 2016, 7(47):77683-77695
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
S7357 PF-562271 HCl PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
J Exp Clin Cancer Res, 2021, 40(1):364
Cancers (Basel), 2021, 13(24)6344
Nat Commun, 2020, 11(1):3282
S7653 PND-1186 (VS-4718) PND-1186 (VS-4718, SR-2156) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Int J Mol Sci, 2022, 23(2)833
J Exp Clin Cancer Res, 2021, 40(1):364
J Exp Clin Cancer Res, 2021, 40(1):91
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Theranostics, 2022, 12(3):1097-1116
Cell Death Dis, 2022, 13(1):54
Nat Commun, 2021, 12(1):3904
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Mol Cell, 2021, S1097-2765(21)00264-1
Sci Signal, 2021, 14(682)eabc1648
Biochem Pharmacol, 2021, S0006-2952(21)00185-4
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
Biomaterials, 2021, 279:121235
Int J Mol Sci, 2021, 22(2)E752
J Neurosci Methods, 2021, 356:109141
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