k(2p)

Ropivacaine hydrochloride (Ropivacaine monohydrochloride) is the hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

RU-TRAAK-2 is a reversible inhibitor of TWIK-related arachidonic acid-stimulated K+ channel with no activity for non-K2P channels including Kv1.2, GIRK2, and Slo1.

PND-1186 (VS-4718) is a small molecule inhibitor, a highly specific, reversible FAK inhibitor (IC50=1.5 nM) with good selectivity and cell permeability. This compound inhibits FAK phosphorylation, blocking tumor cell survival, proliferation, migration, and angiogenesis, and is primarily used for anti-tumor research on solid tumors.

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

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.

BI-4464 is a highly selective inhibitor targeting focal adhesion kinase (FAK). BI-4464 effectively blocks the catalytic activity of FAK by competitively binding to the ATP-binding site, with an IC₅₀ of 17 nM. In addition to its role as a kinase inhibitor, BI-4464 can also serve as a FAK-targeting ligand (warhead) for PROTAC design. By conjugation with an E3 ligase ligand via an appropriate linker, the resulting PROTAC molecule can induce the selective degradation of FAK through the ubiquitin–proteasome pathway, providing a valuable tool for cancer biology and related disease research.

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

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

CK2/PIM1-IN-1 is an inhibitor of CK2 (IC50: 3.787 μM) and PIM1 (IC50: 4.327 μM), developed for researching proliferative disorders like cancer and other kinase-associated conditions.

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

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.

CDK2/PIM1-IN-1 is an inhibitor of the kinases CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM). It can induce apoptosis (cell death) and reduce the expression of TNF-α, which promotes tumors. CDK2/PIM1-IN-1 exhibits antitumor activity.

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.

PROTAC CDK2-pRb degrader-1 is an orally bioavailable degrader belonging to the PROTAC class, specifically targeting CDK2/cyclin E complexes. It functions by promoting the ubiquitination and proteasomal degradation of CDK2, thereby effectively inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811. PROTAC CDK2-pRb degrader-1 demonstrates significant activity in human cells with EC50 values of 12 nM and 125 nM. In xenograft models, it inhibits tumor growth and induces tumor stasis, making it suitable for research on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers.

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).