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GSK215 is a potent and selective PROTAC focaladhesionkinase (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 .
Y15 is a potent and specific inhibitor of focaladhesionkinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
PF-431396 is an orally active dual focaladhesionkinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively .
FAK-IN-3 (Compound 36) is a potent inhibitor of focaladhesionkinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer .
Antitumor agent-165 (Compound 10l) is a potent focaladhesionkinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM .
FAK-IN-16 (compound OXA-11) is an orally active, selective focaladhesionkinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
GSK-2256098 hydrochloride is a focaladhesionkinase (FAK) inhibitor that exhibits potential antiangiogenic and antineoplastic activities. GSK-2256098 hydrochloride targets FAK to inhibit tumor cell growth by regulating cell adhesion, migration, proliferation, and survival.
Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focaladhesionkinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM) .
FAK-IN-17 is a focaladhesionkinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
Ifebemtinib (BI 853520) is an orally active and potent focaladhesionkinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. Petunidin chloride binds with and suppresses the activity of focaladhesionkinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.
FAK-IN-15 (Compound 9b) is a focaladhesionkinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells .
FAK-IN-2 is a potent and orally active focaladhesionkinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
FAK-IN-14 (compound 8d) is a focaladhesionkinase(FAK) inhibitor with an IC50 value of 0.2438 nM. FAK-IN-14 induces U87-MG cell early apoptosis and arrest the cell at the G2/M phase .
Petunidin (chloride) (Standard) is the analytical standard of Petunidin (chloride). This product is intended for research and analytical applications. Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. Petunidin chloride binds with and suppresses the activity of focaladhesionkinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focaladhesionkinase (FAK) and Src. YF-452 is a potential antiangiogenic agent candidate for cancer research .
Narmafotinib (AMP-945) is an inhibitor of the enzyme focaladhesionkinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells) .
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focaladhesionkinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively .
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focaladhesionkinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
ZINC40099027 is a FAK activator. ZINC40099027 promotes FAK phosphorylation, inducing mucosal healing in murine models. ZINC40099027 can be used for Gastroduodenal ulcer disease research .
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focaladhesionkinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focaladhesionkinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
proMMP-9 inhibitor-3c (compound 3c) is a potent proMMP-9 inhibitor. proMMP-9 inhibitor-3c is specific for binding to the proMMP-9 hemopexin-like domain (Kd=320 nM). proMMP-9 inhibitor-3c disruption of MMP-9 homodimerization prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR. This disruption results in decreased phosphorylation of Src and its downstream target proteins focaladhesionkinase (FAK) and paxillin (PAX) .
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focaladhesionkinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
PH11 is a novel focaladhesionkinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
LB Broth Base, powder (Luria-Bertani Base) is generally used to maintain the growth of E. coli. The composition of 1 liter of LB medium is: 10 g peptone, 5 g yeast extract and 5 g NaCl .
Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. Petunidin chloride binds with and suppresses the activity of focaladhesionkinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focaladhesionkinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
Petunidin (chloride) (Standard) is the analytical standard of Petunidin (chloride). This product is intended for research and analytical applications. Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. Petunidin chloride binds with and suppresses the activity of focaladhesionkinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.
Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focaladhesionkinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
FAK1 is a nonreceptor protein tyrosine kinase that coordinates multiple cellular processes. FAK1 Protein, Human (Sf9, GST) is the recombinant human-derived FAK1 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of FAK1 Protein, Human (Sf9, GST) is 1052 a.a., .
Phospho-FAK (Tyr576) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 119 kDa, targeting to Phospho-FAK (Tyr576). It can be used for WB assays with tag free, in the background of Human, Mouse.
PYK2 Antibody (YA682) is a non-conjugated and Mouse origined monoclonal antibody about 116 kDa, targeting to PYK2 (4B4). It can be used for WB,IHC-P assays with tag free, in the background of Human.
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