FAK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

FAK Products

New FAK Products
Catalog No. Information Product Use Citations Product Validations
S2672

PF-00562271 Besylate

PF-00562271 Besylate 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.

S2890

PF-562271

PF-562271 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.

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.

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.

S2725

PF-03814735

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

S5321New

Y15

Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.

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.

S8523

GSK2256098

GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM.

S7653

PND-1186 (VS-4718)

PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.

S7644

PF-431396

PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.

S7654

Defactinib (VS-6063, PF-04554878)

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

S2360

Solanesol (Nonaisoprenol)

Solanesol 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.

Catalog No. Information Product Use Citations Product Validations
S2672

PF-00562271 Besylate

PF-00562271 Besylate 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.

S2890

PF-562271

PF-562271 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.

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.

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.

S2725

PF-03814735

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

S5321New

Y15

Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.

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.

S8523

GSK2256098

GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM.

S7653

PND-1186 (VS-4718)

PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.

S7644

PF-431396

PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.

S7654

Defactinib (VS-6063, PF-04554878)

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

S2360

Solanesol (Nonaisoprenol)

Solanesol 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