FAK

Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

FAK PROTAC B5: a degrader with 14.9 nM IC50, strong degradation, anti-growth, good plasma stability, and fair permeability.

FAK-IN-1 is a FAK inhibitor with anticancer activities (WO2020231726 (Example 27)).

FAK-IN-11 (Compound 4l), a FAK inhibitor, specifically targets the ATP binding pocket of FAK to prevent its phosphorylation.

Ifebemtinib (BI-853520) hydrochloride is a potent FAK (focal adhesion kinase) inhibitor with oral bioavailability, exhibiting an IC50 of 1 nM for recombinant FAK. Ifebemtinib hydrochloride demonstrates antiproliferative activity against cancer cells.

FAK-IN-12 (Compound 12S) is a selective FAK inhibitor with an IC50 of 47 nM.

FAK-IN-15 is a highly potent focal adhesion kinase (FAK) inhibitor with antitumor activity.

FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.

A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related

Adhesamine diTFA, a dumbbell-shaped molecule, activates the MAPK/FAK pathway. It promotes adhesion and growth in mammalian cells and accelerates differentiation and enhances the survival rate of primary cultured mouse hippocampal neurons.

MLK3-IN-1 (Compound 37) is a selective inhibitor of mixed-lineage kinase 3 (MLK3) with an IC50 of less than 1 nM. It also inhibits FAK with an IC50 of 15.5 μM. In both murine and human liver microsomes, MLK3-IN-1 demonstrates excellent metabolic stability.

MY-1576 is a FAK inhibitor with an IC50 of 8 nM. It activates the Hippo pathway, thereby inhibiting YAP/TAZ regulation. Additionally, MY-1576 effectively suppresses tumor growth in the KYSE30 xenograft mouse model, demonstrates good safety, and efficiently downregulates FAK autophosphorylation and YAP/TAZ levels in vivo.

Lewis Y tetrasaccharide, a derivative of Lewis X, is an antigen linked to ovarian cancer metastasis and bad prognosis.

Compound 2119738-71-3 interacts with the FAK receptor.

FAK-IN-9 (8f) is a potent oral FAK inhibitor, IC50 of 27.44 nM; induces TNBC cell apoptosis.

VnP-16 enhances bone formation by stimulating the differentiation and activity of osteoblasts via direct β1 integrin engagement, which subsequently activates

Body Protection Compound 157 (BPC 157) is a pentadecapeptide derived from BPC, identified in gastric juice, exhibiting diverse biological activities. At 2 µg/ml, BPC 157 enhances primary rat tendon fibroblast cell migration and F-actin formation. Furthermore, doses of 0.01 and 10 µg/kg, intraperitoneally (i.p.), mitigate paw swelling, bone erosion, and mononuclear cell infiltration in the joints of rats with rheumatoid arthritis induced by complete Freund's adjuvant (CFA). It also diminishes gastric ulcer size in rats caused by indomethacin, aspirin, or diclofenac at these doses. Additionally, BPC 157 reduces catalepsy duration and tremor severity in a mouse model of Parkinson's disease triggered by MPTP.

PROTACFAKdegrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). It induces FAK degradation through the ubiquitin-proteasome system and its interaction with FAK and CRBN. By inhibiting FAK's non-catalytic activity, PROTACFAKdegrader 3 enhances MHC-I gene transcription and tumor cell surface expression, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. Its ability to promote MHC-I expression and boost T cell activation strengthens its antitumor efficacy in vivo. PROTACFAKdegrader 3 is applicable to cancer research targeting FAK degradation, including studies on ovarian cancer and hepatocellular carcinoma.

BI-853520 FA (Ifebemtinib FA) is an orally active inhibitor of adhesion patch kinase with anticancer and antiproliferative activity for ovarian and lung cancer.

FAK-IN-27 (compound 8A) is a potent and selective inhibitor of FAK, with an IC50 of 4.968 nM. It effectively inhibits the proliferation of H1299 cells, with an IC50 of 0.28 μM, and is applicable for research in non-small cell lung cancer (NSCLC).

FAK-IN-10 is an inhibitor of FAK (IC50:76.3 μM).FAK-IN-10 z MCF-7 and A431 cell lines showed antitumor activity with IC50 of 4.23 and 0.78 μM, respectively.

Defactinib analogue-1 (Compound 7) serves as a ligand for the target protein FAK, and is utilized in the synthesis of PROTAC FAK degrader 1.

GSK215: potent, selective PROTAC degrader of FAK (pDC50=8.4), combines FAK inhibitor VS-4718 and VHL E3 ligase binder, causes fast, lasting FAK degradation.

Anti-PTK2 Antibody (4T687) is an antibody targeting PTK2. Anti-PTK2 Antibody (4T687) can be used in ELISA, IHC.

Conteltinibtetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride form of Conteltinib. It acts as an inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. When used in combination with Cabozantinib, Conteltinib tetrahydrochloride exhibits a synergistic antitumor effect.

BI-3663 is a selective PTK2/FAK PROTAC with cereblon ligands, degrading PTK2 (IC50: 18 nM), and shows anti-cancer properties.

Defactinib (VS-6063) is a second-generation inhibitor of FAK. Defactinib has potential antitumor activity. Cost-effective and quality-assured.

SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs.

Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity,

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

Fangchinoline (Tetrandrine B) is extracted from Stephania tetrandra S. Moore.

AMP-945 is a proprietary focal adhesion kinase (FAK) inhibitor.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK.

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

1.

<p>BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC</p>

Batatasin III inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition and FAK-AKT signals and possesses anti-cancer

GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.

NVP-TAE 226: Potent FAK inhibitor, IC50=5.5nM, stronger vs Pyk2, IC50=3.5nM, weaker against IGF-1R, InsR, c-Met, ALK.

PF-562271 besylate: potent, ATP-competitive FAK inhibitor, IC50 1.5 nM, 10x less effective on Pyk2, highly selective vs other kinases.

PND-1186 (VS-4718) is a reversible and specific FAK inhibitor (IC50: 1.5 nM).

CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

<p>ZINC40099027 is a FAK activator that induces gastric mucosal repair in persistent aspirin-associated gastric injury.</p>

PF-719 is a potent, selective Pyk2 inhibitor with IC50 of 17 nM.

PH11, a FAK inhibitor, reactivates TRAIL apoptosis in PANC-1 cells by reducing c-FLIP and inhibiting FAK/PI3K/AKT.

focal adhesion kinase (FAK) inhibitor

FAK inhibitor 2, antitumor and anti-angiogenesis activitiesis ,is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM .

FAK-IN-8 (compound 5h), a FAK inhibitor with an IC50 of 5.32 μM, exhibits potent anti-proliferative activity, making it suitable for use in cancer research [1].

FAK inhibitor 5 is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.

ProMMP-9 inhibitor-3c hinders MMP-9 homodimers, blocks proMMP-9/α4β1 integrin/CD44 binding, and detaches EGFR.

Adhesamine, a dumbbell molecule, enhances cell adhesion, growth, neuron differentiation, and survival via MAPK/FAK.

FLT3-IN-17: FAK inhibitor, IC50 of 12 nM; blocks CYPs, FLT3 mutants; IC50 <0.5 nM for D835Y in cancer studies.

TG53 is a tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction inhibitor.

NAMI-A is a ruthenium-based compound with selective activity against tumor metastasis.NAMI-A inhibits cancer cell adhesion and migration.

Defactinib hydrochloride (PF 04554878 hydrochloride) is a novel inhibitor of FAK.

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5.

FC 11 is a reversible FAK PROTAC Degrader with DC50 of 40-370 pM and degrades pFAKtyr397 in TM3 cells within 3 hours at 100 nM.

Ifebemtinib (BI-853520) is an adhesion plaque kinase inhibitor with anti-tumour activity for the study of breast cancer.

FAK-IN-6: Potent FAK inhibitor (IC50=1.415 nM), anti-cancer, for pancreatic studies.

<p>FAK-IN-26 is a blood-brain barrier-penetrating inhibitor of Focal Adhesion Kinase (FAK) with an IC50 of 0.87 nM. It significantly reduces tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 exhibits potent anticancer activity, achieving tumor inhibition rates of 59.15% and 57.9% in A549 and SKOV-3 tumor mouse models, respectively.</p>

Pyk2-IN-2 (compound 13j) acts as a Pyk2 inhibitor, exhibiting an IC 50 value of 0.608 μM for FAK kinase [1].

FAK-IN-21 (compound 9) is a FAK inhibitor with an IC50 value of 37.52 nM. It inhibits cell growth and the phosphorylation of FAK, making it useful for research into diffuse gastric cancer.

JP-153 is an inhibitor of Src-FAK-Paxillin signaling. It suppresses Src-dependent phosphorylation of paxillin (Y118) and subsequent activation of Akt (S473). JP-153 reduces VEGF-induced migration and proliferation of retinal endothelial cells and is applicable in the study of neovascular eye diseases.

OXA-11 (FAK-IN-16) is a FAK inhibitor with anti-tumor activity, useful for cancer research.

<p>FAK-IN-23 (Compound II) is an inhibitor of focal adhesion kinase (FAK).</p>

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor with anti-tumor properties. It inhibits FAK autophosphorylation in prostate cancer cells and suppresses spheroid formation and in situ tumor growth in vivo. Ifebemtinib (tosylate) is applicable in cancer research, including studies on solid tumors, breast cancer, and malignant pleural mesothelioma.

Compound 26F: potent enzyme inhibitor (IC50=28.2nM), low cytotoxicity (IC50=3.32μM), induces dose-dependent apoptosis in MDA-MB-231, blocks G0/G1 phase.

<p>FAK-IN-3 inhibits FAK, reduces PA-1 cell migration/invasion, and tumor growth, with no major side effects.</p>