Cat.No. | Name | Information |
---|---|---|
M2931 | PF-573228 | PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
M2302 | PF-562271 | PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. |
M29789 | GSK215 | GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect. |
M21138 | AMP-945 | AMP945 is an inhibitor of focal adhesion kinase (FAK), an enzyme that plays a key role in the formation of scar tissue (fibrosis) in diseases such as cancer and IPF. |
M14893 | PND-1186 hydrochloride | PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis. |
M10508 | BI-4464 | BI-4464 is a novel highly selective ATP competitive inhibitor of PTK2/FAK with IC50 of 17 nM, it is also a PTK2 ligand for PROTAC. |
M9256 | Solanesol | Solanesol (Nonaisoprenol) is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. |
M8945 | Defactinib hydrochloride | Defactinib hydrochloride is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. |
M6139 | GSK2256098 | GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. |
M5347 | Y15 | Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK. |
M5334 | PF-431396 | PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively. |
M4978 | PND-1186 | PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. |
M4872 | Defactinib | Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. |
M3286 | PF-00562271 | PF-00562271 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. |
M2301 | NVP-TAE226 | Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. |
M29603 | FAK inhibitor 6 | Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase. |
M29180 | PDZ1i | PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion. |
M28276 | YH-306 | YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization. |
M27986 | Ifebemtinib | Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. |
M27874 | PF-4618433 | PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration. |
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