FAK

FAK Products

  • All (18)
  • FAK Inhibitors (17)
  • FAK Activator (1)
  • New FAK Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
Cell Rep, 2023, 42(5):112529
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.
Bioact Mater, 2023, 20:598-609
Nat Commun, 2023, 14(1):6777
Cancers (Basel), 2023, 15(13)3379
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Clin Cancer Res, 2024, 30(1):187-197
Signal Transduct Target Ther, 2023, 8(1):11
Gut, 2023, gutjnl-2022-327927
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.
J Exp Med, 2023, 220(9)e20230054
Adv Sci (Weinh), 2023, 10(10):e2205397
J Thromb Haemost, 2023, 21(8):2236-2247
S7653 VS-4718 (PND-1186) VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Cell Death Dis, 2024, 15(2):108
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
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
S2672 PF-562271 Besylate PF-562271 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
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
Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
Cancer Res Treat, 2022, 54(3):767-781
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.
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
Research (Wash D C), 2023, 6:0215
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
Nat Commun, 2023, 14(1):6270
Cell Rep, 2023, 42(5):112529
J Exp Clin Cancer Res, 2021, 40(1):364
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.
Cells, 2023, 12(15)1964
J Cell Sci, 2023, 136(15)jcs261001
Int J Biol Sci, 2022, 18(13):5019-5037
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
E0806 Narmafotinib Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E3677 Semen Ziziphi Spinosae Extract Semen Ziziphi Spinosae Extract is extracted from the seeds of Semen Ziziphi Spinosae, which can attenuate blood-brain barrier dysfunction induced by lipopolysaccharide by targeting the FAK-DOCK180-Rac1-WAVE2-Arp3 signaling pathway.
E1113 GSK215 GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader, which exerts FAK degradation in A549 non-small-cell lung cancer cells with DC50 of 1.3 nM by a strong time-dependence way and maximal degradation (Dmax) near the limit of the assay quantification (Dmax 99%).
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
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.
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.
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
Cell Rep, 2023, 42(5):112529
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.
Bioact Mater, 2023, 20:598-609
Nat Commun, 2023, 14(1):6777
Cancers (Basel), 2023, 15(13)3379
S7654 Defactinib (VS-6063) Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Clin Cancer Res, 2024, 30(1):187-197
Signal Transduct Target Ther, 2023, 8(1):11
Gut, 2023, gutjnl-2022-327927
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.
J Exp Med, 2023, 220(9)e20230054
Adv Sci (Weinh), 2023, 10(10):e2205397
J Thromb Haemost, 2023, 21(8):2236-2247
S7653 VS-4718 (PND-1186) VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
Cell Death Dis, 2024, 15(2):108
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
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
S2672 PF-562271 Besylate PF-562271 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
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
Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119
Cancer Res Treat, 2022, 54(3):767-781
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.
Gut, 2023, gutjnl-2022-327927
Gut, 2023, 1–2
Research (Wash D C), 2023, 6:0215
S7644 PF-431396 PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
Nat Commun, 2023, 14(1):6270
Cell Rep, 2023, 42(5):112529
J Exp Clin Cancer Res, 2021, 40(1):364
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.
Cells, 2023, 12(15)1964
J Cell Sci, 2023, 136(15)jcs261001
Int J Biol Sci, 2022, 18(13):5019-5037
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
S6545 BI-4464 BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM.
E0806 Narmafotinib Narmafotinib (AMP-945) is an inhibitor of focal adhesion kinase (FAK).
E1113 GSK215 GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader, which exerts FAK degradation in A549 non-small-cell lung cancer cells with DC50 of 1.3 nM by a strong time-dependence way and maximal degradation (Dmax) near the limit of the assay quantification (Dmax 99%).
E0814 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK.
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.
E3677 Semen Ziziphi Spinosae Extract Semen Ziziphi Spinosae Extract is extracted from the seeds of Semen Ziziphi Spinosae, which can attenuate blood-brain barrier dysfunction induced by lipopolysaccharide by targeting the FAK-DOCK180-Rac1-WAVE2-Arp3 signaling pathway.

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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