ptk2

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

Defactinib (VS-6063) is a second-generation inhibitor of FAK that inhibits FAK phosphorylation at the Tyr397 site. Defactinib has potential antitumor activity.

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

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

Batatasin III inhibits cancer migration and invasion by suppressing epithelial to mesenchymal transition and FAK-AKT signals and possesses anti-cancer activities. Batatasin III has a long-term inhibitory effect on whole-plant growth and shows germination

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

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

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

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

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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

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

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

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition, crucial in synthesizing various PROTACs, including BI-3663, a selective PTK2 FAK PROTAC. Using cereblon ligands, it targets E3 ligases to degrade PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1].

BI-3663 is a highly selective PTK2 FAK PROTAC that utilizes cereblon ligands to hijack E3 ligases for PTK2 degradation, with an IC50 of 18 nM. It is composed of BI-4464 linked to Pomalidomide with a linker[1]. Anti-cancer.

PF-562271 hydrochloride (PF-562271 HCl) 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.

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 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).

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

TL13-22 is a potent inhibitor of Anaplastic Lymphoma Kinase (ALK) with an IC₅₀ value of 0.54 nM and does not lead to degradation of ALK proteins.TL13-22 is often used as a negative control for TL13-12 (induces ALK protein degradation) as a negative control.TL13-22 also induces degradation of other kinases, including Aurora A, FER, PTK2, and RPS6KA1.

BI-4464, a highly selective ATP-competitive inhibitor of PTK2 FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

1. Nitidine chloride has inhibitory effects on various tumors, such as renal cancer , breast cancer. 2. Nitidine chloride inhibits the proliferation of SMMC-7721 cells in vitro in a time- and dose-dependent manner and identifies efficacy in vivo in a mouse model of HCC.