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. |
|
|