focal

Orotirelin(CG 3509), a thyrotropin-releasing hormone analog, reversed pentobarbital-induced sleep time.Orotirelin may be beneficial in animals with focal cerebral ischemia.

pp60 c-src (521-533) (phosphorylated) acetate is a regulator of focal adhesion formation and cell spreading. pp60 c-src (521-533) (phosphorylated) acetate also regulates cell motility and is a key component in the signaling pathway triggered by the motogenic hyaluronan receptor RHAMM.

FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells.

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

Antroquinonol is a ubiquinone derivative from Antrodia camphorata with anti-inflammatory and anticancer activities.Antroquinonol reduces oxidative stress and inhibits inflammation and sclerosis in mice with focal segmental glomerulosclerosis through enhancement of the Nrf2 signaling pathway.Antroquinonol has potential for use in the treatment of non-small cell lung cancer. Antroquinonol has potential for the treatment of non-small cell lung cancer and may be used in colon cancer research.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

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

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

Morroniside would act as a regulator of hepatic inflammatory reactions and lipid metabolism in db/db mice. It exhibits protective effects against diabetic renal damage and human umbilical vein endothelial cells, by inhibiting hyperglycemia and oxidative s

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

NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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

Defactinib (VS-6063) is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

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

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

Fresolimumab (GC1008) is a specific human anti-transforming growth factor β monoclonal antibody that binds to the active forms of human TGFβ1, TGFβ2, and TGFβ3 and can be used to study focal segmental glomerulosclerosis and cancer in adults.

Gadobutrol is a medicinal product used in diagnostic magnetic resonance imaging (MRI) in adults and children. It provides contrast enhancement during cranial, spinal, breast, or other investigations. In the central nervous system, Gadobutrol works by high

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 FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).

NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

LY 215490 is a selective, competitive and systemically active antagonist of AMPA receptor. LY 215490 has neuroprotective effect against focal ischaemia in a model of permanent MCA occlusion in the rat.

Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.

Emodin-8-glucoside (Anthraglycoside B) functions to protect from focal cerebral injury induced by ischemia and reperfusion. Emodin-8-beta-D-glucoside directly stimulates cell proliferation and differentiation of osteoblasts.

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 1 is a selective ALK kinase inhibitor.

Gadoxetate Disodium is used to evaluate focal liver lesions, such as hepatocellular carcinoma or liver metastasis on T1-weighted imaging. It is a contrast agent in magnetic resonance imaging (MRI) of the hepatobiliary system. It accumulates in normal, fun

Ilacirnon sodium is a potent CCR2 antagonist that may be useful in the treatment of renal diseases including Focal Segmental Glomerulosclerosis and Diabetic Nephropathy.

APOL1-IN-1 is a potent inhibitor of apolipoprotein L1 (APOL1) that can be used to study the pathogenesis of focal segmental glomerulosclerosis (FSGS) and nondiabetic kidney disease (NDKD), facilitating research into these diseases.

COVID-19 Spike Protein mRNA-LNP is a lipid nanoparticle (LNP) formulated with the novel coronavirus pneumonia spike protein, positioned on the membrane surface, designed for applications such as RNA delivery, translation efficiency, and cell viability assessment. This spike protein facilitates the COVID-19 virus's entry into host cells by binding to cell membrane receptors and enabling membrane fusion, making it a critical focal point for host neutralizing antibodies and vaccine development [1].

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

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.

Potent and noncompetitive NMDA receptor antagonist (IC50 = 36 nM). Exhibits >70-fold selectivity for NMDA receptor over σ receptor. Neuroprotective in a rat model of focal ischemia.

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4). GSK215 is designed by the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase. GSK215 can induce rapid and prolonged FAK degradation.

Gardenin has regulatory effect on the gene expression in rats with focal cerebral ischemia.

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

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.

Water-soluble salt of lamotrigine . Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Leach et al (1991) Neurochemical and behavioral aspects of lamotr. Epilepsia 32 S4 PMID:1685439 |Smith and Meldrum (1995) Cardioprotective effect of lamotr. after focal ischemia in rats. Stroke 26 117 PMID:7839380 |Zona and Avoli (1997) Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture. Epilepsia 38 522 PMID:9184596 |Grunze et al (1998) Modulation of calcium and potassium currents by lamotr. Neuropsychobiology 38 131 PMID:9778600

L-NIO dihydrochloride, a potent and non-selective NADPH-dependent nitric oxide synthase (NOS) inhibitor, consistently induces focal ischemic infarct in rats. It exhibits inhibitory constants (Kis) of 1.7, 3.9, and 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS) forms, respectively.

Lamotrigine hydrate is an effective oral active anticonvulsant or antiepileptic agent that selectively blocks voltage-gated Na + channels, stabilizes presynaptic neuronal membranes and inhibits glutamate release. Lamotrigine hydrate can be used in epilepsy, focal seizure, et al [1] [2].

Azurin (50-77) is a peptide fragment derived from the copper-containing bacterial protein azurin, present in P. aeruginosa. It exhibits properties that regulate the cell cycle, inhibit cancer proliferation, and manage angiogenesis, proving its potential as an anticancer agent. Specifically, this compound acts as a VEGFR2 inhibitor with an IC20 of approximately 10.7 µM. At a concentration of 20 µM, it effectively induces cell cycle arrest at the G2/M phase in MCF-7 breast cancer cells, while a higher concentration of 50 µM significantly reduces the proliferation of both MCF-7 and ZR-75-1 breast cancer cell lines. Furthermore, Azurin (50-77) impedes VEGF-A-induced capillary tube formation with an IC50 of 12 µM, and alters the cellular and extracellular levels of critical signaling and structural proteins such as F-actin, focal adhesion kinase (FAK), paxillin, and platelet endothelial cell adhesion molecule-1 (PECAM-1) in human umbilical vein endothelial cells (HUVECs) at a concentration of 25 µM. Demonstrating its efficacy in vivo, Azurin (50-77) administered at 10 mg/kg per day notably reduces tumor volume in an MCF-7 mouse xenograft model, highlighting its therapeutic potential.

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

HCV Core Protein (107-114), identified as the binding site within the region 101-118, is a minimally immunogenic fragment of the primary linear HCV core regions. This segment, comprising two residues that vary between genotypes I/II and III/VI, represents a potential focal point for the dissemination of HCV serotypes [1].

Methsuximide is an anticonvulsant agent which appeared to be effective in petit mal, psychomotor and focal motor attacks [1].

NAT, an initial NAMPT activator, targets NAMPT, a crucial enzyme in the NAD salvage pathway and a key focal point for researching a variety of diseases linked to NAD depletion, including neurodegenerative diseases[1].

OXA-11 is a potent inhibitor of focal adhesion kinase (FAK) with anti-tumor activity.

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

Oxysophoridine (Sophoridine N-oxide) has a protective effect on focal cerebral ischemic injury through antioxidant and anti-apoptotic mechanisms; it may be a potential neuroprotective agent for cerebral ischemia injury, that the effect may be due to its ability to inhibit oxidative stress and expression of the N-methyl-D-aspartate receptor subunit NR1.Oxysophoridine ameliorates cardiac damage in a rat model of AMI and that this cardioprotection may be linked with its anti-oxidative, anti-apoptotic and anti-inflammatory properties.

GSK-2256098 HCl is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

Moexipril methyl ester is a long-acting, non-sulfhydryl angiotensine-converting enzyme inhibitor.

Moexipril is an orally active angiotensin-converting enzyme (ACE) inhibitor that readily penetrates lipid membranes, targets plasma and tissue ACE, improves endothelial dysfunction, has neuroprotective activity, and can be used in the study of cardiovascular disease.

Moexipril hydrochloride (Moexipril HCl) is a potent orally active nonsulfhydrylangiotensin converting enzyme (ACE)inhibitor, used for the treatment of hypertension and congestive heart failure.