Fangchinoline is a phytochemical that has been shown to elicit anti-cancer effects in prostate and breast cancer cell lines via inducing G1 cell cycle arrest. It has also been shown to possess neuroprotective activity.
Petunidin chloride is an O-methylated anthocyanidin derived fromdelphinidinthat imparts blue-red pigments to flowers, fruits, and red wine. Petunidin chloride binds with and suppresses the activity offocal adhesion kinase and to inh...
Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner.
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.
In vitro: NAMI-A can significantly affect tumor cells with metastatic ability.
PF-562271 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 CD...
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.
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.
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novelFAKinhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect onFAKwith an IC50 of 1.6nM.
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
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