Organometallic Ligands

<p>The sequence of this peptide has been derived from a highly conserved region of the T-cell phosphatase TC.PTP45 and is an excellent general substrate for protein tyrosine phosphatases.The protein tyrosine phosphatase (PTP) superfamily has 103 enzymes that catalyse substrate dephosphorylation at tyrosine residues through a covalent enzyme intermediate involving a thiophosphate linkage from the active site cysteine residue. All PTPs share a common signature motif (I/V)HCXAGXGR(S/T), named the P-loop, responsible for the enzyme activity. The PTP superfamily can be divided into four classes based on their cellular localization/catalytic domains: the receptor-like PTPs (rPTPs), the non-receptor PTPs (nrPTPs), the low molecular weight PTP (LMWPTP), and the VH-1 and CDC-25 groups.PTPs are involved in regulating a plethora of cellular activities, including proliferation and differentiation, survival, migration, metabolism, and the immune response. Abnormal protein tyrosine phosphorylation has been associated with the etiology of various human diseases, including cancer, diabetes, and autoimmune dysfunctions, therefore making PTPs novel therapeutic targets.</p>

<p>During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-56 predominantly contained 3 peptides - SDNRNQGY, KGLWE, and IQVPL. KGLWE in EYGF-56 was found to have very strong antioxidant activity. KGLWE showed minimal angiotensin converting enzyme (ACE) inhibitory activity.</p>

<p>BX471 hydrochloride is a selective antagonist of the C-C chemokine receptor type 1 (CCR1), which is synthesized through rigorous chemical processes. It operates by inhibiting the binding of chemokines to the CCR1 receptor, thus interfering with the signaling pathways that lead to inflammation and immune responses. This mechanism is specifically effective in modulating immune system functions and controlling pathophysiological responses in various tissue types.</p>

<p>This peptide is phosphorylated by Janus kinase 1 (JAK1) and is an ideal substrate for use in kinase assays. The JAK family of kinases is essential for the signalling of a host of immune modulators in tumour, stromal, and immune cells where they are highly expressed. JAK family proteins mediate the signalling of the interferon (IFN), IL-6, and IL-2 families of cytokines.JAK kinases are associated with cytokine receptors. Cytokine binding to these receptors results in activation of JAK kinases and receptor phosphorylation. Phosphorylated cytokine receptors recruit STAT proteins, which are then phosphorylated by the activated JAK kinases. Phosphorylated STAT proteins form homo- and hetero-dimers that translocate into the nucleus and function as transcription factors.This JAK1 substrate peptide contains an N-terminal Glycine-residue and a phospho-tyrosine-residue.</p>

<p>A15 also known as alpha2-Antiplasmin is a serine/protease inhibitor which inactivates plasmin in the blood. To inhibit plasmin in the blood alpha2-Antiplasmin forms a protease serpin complex with plasmin due to interactions of kringle 1 or 3 of plasmin and the lysine residues of alpha2-Antiplasmin's C-terminus. Although synthesised in the Liver A15 is also present within the neurons of the human brain and its expression has been found to be enhanced in Aβ plaques of Alzheimer's disease and during myocardial infarction. A high concentration of alpha2-Antiplasmin in the blood may also contribute to an increased risk of Ischemic strokes. Alternatively its expression appears to be diminished in patients with cirrhosis and acute liver failure. A further function of A15 is its ability to regulate fibrinolysis through crosslinking to fibrin.</p>

<p>Protein kinase B (also known as RAC-alpha serine/threonine-protein kinase: Atk) is a serum and glucocorticoid-regulated protein kinase with three highly homologous isoforms (Akt1, 2 and 3). Akt1 and Akt3 are the predominant isoforms expressed in the brain, whereas Akt2 is mainly expressed in skeletal muscle and embryonic brown fat. These proteins play major regulatory roles in a range of physiological processes including: growth, proliferation, cell survival, angiogenesis, metabolism and Akt is also considered a proto-oncogene.This peptide (AKTide) is a selective substrate for these kinases and enables quick, easy and sensitive assays of Akt activity.</p>

<p>NMDA glutamate receptor antagonist; anti-depressant</p>

<p>Vitamin B6 antimetabolite</p>

<p>Tolvaptan is a vasopressin receptor antagonist. It binds to the V2 receptor in the cytosol and prevents it from activating the aquaporin 2 channel, which regulates water permeability. Inhibition of vasopressin receptors in the kidneys improves fluid and electrolyte balance. Tolvaptan has been shown to be effective for treating congestive heart failure, as well as other disorders that are associated with fluid retention, such as renal dysfunction and metabolic syndrome. Tolvaptan can also be used in combination therapy with other drugs to treat these conditions.</p>

<p>FP prostaglandin receptor agonist</p>

<p>Amlodipine is a calcium channel blocker that is used to treat hypertension and angina. This drug inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle.</p>

<p>Antagonist of Smoothened GPCR; antineoplastic</p>

<p>Roflumilast is a selective phosphodiesterase-4 inhibitor that is used for the treatment of exacerbations in patients with chronic obstructive pulmonary disease (COPD). It is also used to treat plaque psoriasis. This drug has anti-inflammatory and immunomodulatory effects as it aids in increasing levels of cAMP.</p>

<p>Inhibitor of myosin?II?specific ATPase which blocks the myosin heads in an actin-detached state, disrupts contractility of myosin-actin filaments and stabilizes super-relaxed state of muscle fibres. It inhibits skeletal muscle myosin, non-muscle myosin II and heart muscle myosin.</p>

<p>Potent inverse agonist of peroxisome proliferator-activated receptor PPARβ and PPARδ with IC50 value of 27 nM. In mouse myoblasts, DG 172 enhanced recruitment of transcriptional corepressor and down-regulated transcription of PPARβ/δ target gene Angptl4. DG 172 also possess a PPARβ/δ-independent activity on bone marrow cells and promotes dendritic cell differentiation.</p>

<p>Proteosome inhibitor; antineoplastic</p>

<p>Glucocorticoid receptor agonist; anti-inflammatory; immunosuppressant</p>

<p>Esmolol is a beta-adrenergic blocker that is used for the control of heart rate in various types of tachycardia. This drug inhibits the agonistic effect of sympathetic neurotransmitters by binding to the receptor sites. This drug is said to be cardioselective and targets beta-1 receptors.</p>

<p>Pamidronic acid is a bisphosphate used in the treatment of Paget’s disease, osteolytic bone lesions and in the treatment of hypercalcemia of malignancy. This drug inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells.</p>

<p>Mildly inhibits tau protein fibril formation; enhances cognitive function</p>

<p>Inhibits P-gp transporters ; modulates P-gp-mediated multidrug resistance</p>

<p>AZD9833 is an oral selective estrogen receptor degrader (SERD), which is a small molecule therapeutic synthesized by AstraZeneca. Its mode of action involves binding to the estrogen receptor, leading to the receptor's conformational change and subsequent degradation. This mechanism significantly downregulates estrogen receptor signaling, which is a crucial pathway in the progression of estrogen receptor-positive breast cancers.</p>

<p>Cis/trans-form of GK 563 [2351820-19-2]</p>

<p>L-type calcium channel blocker</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Inhibitor of EGFR transmembrane receptor</p>

<p>Phosphodiesterase (PDE5, 6, 9 and 11) inhibitor</p>

<p>Nitric oxide donor; anti-anginal agent</p>

<p>MLN 4924 is a selective small molecule that acts as an inhibitor of the Nedd8-activating enzyme. This compound is synthetically derived and functions by inhibiting the conjugation of Nedd8 to cullin proteins. By blocking this pathway, MLN 4924 disrupts the activity of the SCF (Skp, Cullin, F-box containing complex) E3 ubiquitin ligase, leading to an accumulation of proteins that can induce apoptosis and cell cycle arrest.</p>

<p>Irbesartan is an angiotensin II receptor antagonist that is used to treat hypertension and congestive heart failure. It is also used to delay the progression of diabetic nephropathy. This drug works to works to relax smooth muscles and lower blood pressure.</p>

<p>R-(-)-Arundic acid is a chiral compound, which is a derivative of arundic acid specifically designed for enantiomeric purity. It is sourced through synthetic organic chemistry processes, allowing for precise control over its stereochemistry. The mode of action of R-(-)-Arundic acid involves the inhibition of astrocyte activation by modulating the synthesis of certain cytokines and inflammatory mediators. This mechanism provides a neuroprotective effect, making it a valuable tool in the study of neurodegenerative diseases and brain injuries.</p>

<p>Activator of SIRT1 deacetylase</p>

<p>Inhibitor of cyclin dependend kinases</p>

<p>MK-4074 is an acetyl-CoA carboxylase (ACC) inhibitor, which is a compound originally developed by pharmaceutical research entities focusing on metabolic disorders. Acetyl-CoA carboxylase is a key enzyme in the biosynthesis of fatty acids, playing a critical role in the regulation of lipid metabolism. By inhibiting this enzyme, MK-4074 lowers the levels of malonyl-CoA, subsequently reducing fatty acid synthesis and increasing fatty acid oxidation.</p>

<p>Tetrabenazine is a drug that has been used for the treatment of Parkinson's disease. It acts by inhibiting dopamine release and reducing the activity of nerve cells in the brain. Tetrabenazine Bio-X is used to treat dyskinesias, that are abnormal and involuntary muscle movements by inhibiting the monoamine transporter (VMAT2).<br>Tetrabenazine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use."</p>

<p>Please enquire for more information about GB1107 including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>GDF-15, or Growth Differentiation Factor 15, is a cytokine, which is a type of signaling protein. It is primarily sourced from macrophages, but can also be secreted by other tissues such as the liver, heart, and adipose tissue. The protein is part of the transforming growth factor beta (TGF-β) superfamily and is involved in regulating inflammatory and apoptotic pathways.</p>

<p>Inhibits DNA topoisomerase II; antineoplastic; immunomodulatory; antimicrobial</p>

<p>Maleimide-DOTA is a chemical conjugation agent, which is a synthetic compound used in the field of radiopharmaceutical development. It is derived from the combination of maleimide and DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid). The maleimide moiety specifically reacts with thiol groups, allowing for the selective conjugation to cysteine residues of peptides or proteins. This reactivity is crucial for precise coupling in biochemical modifications, while the DOTA component serves as a versatile chelator for radiometals.</p>

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.<br>Sorafenib is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>17:0-20:4 PI (3,4,5) P3 is a synthetic phosphoinositide, a type of lipid molecule, which is typically derived from chemical synthesis using specialized lipid chemistry techniques. This product is designed to mimic natural phosphoinositides found within the cellular membranes. Its mode of action involves acting as a substrate for studying kinase activities and phosphatase interactions within signaling pathways. 17:0-20:4 PI (3,4,5) P3 plays a critical role in cellular signaling by serving as a docking site for signaling proteins with specific lipid-binding domains, influencing downstream signaling pathways.</p>

<p>CBP/p300 histone acetyltransferase activator</p>

<p>Pitolisant is an inverse agonist and antagonist of the histamine (H3) receptor. It acts as an allosteric modulator of the H3 receptor to increase the activity of histamine at the M1 receptor. Pitolisant has been used in the treatment of narcolepsy, schizophrenia and Alzheimer's disease. Its mechanism of action involves binding to the amide group on histamine, which increases its affinity for the H3 receptor and enhances its activity at this site. Pitolisant has been shown to improve cognitive ability and reduce fatigue in patients with Alzheimer's disease.<br>Pitolisant is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Inhibitor of dioxygenase IDO1</p>

<p>Inhibitor of clathrin-mediated endocytosis (CME) and ligand to the clathrin heavy chain (CHC). ES9-17 is an inhibitor of the CHC function with EC50 of 13 μM in plant model Arabidopsis thaliana. ES9-17 is a non-protonophoric CME inhibitor and it does not alter the cytoplasmic pH levels substantially. In a mammalian cell line HeLa, ES9-17 reduced the uptake of transferrin, which is a CME-driven process.</p>

<p>Cisplatin, also known as cisplatinum, is a platinum-based anti-cancer agent that inhibits the EGFR, which is a receptor tyrosine kinase. It has been shown to have anti-cancer effects in melanoma cells and to inhibit tumor growth in mice. Cisplatin acts by interfering with the mechanism of DNA repairing. It loses one chloride ligand and binds to DNA to inhibit the synthesis, causing DNA damage, and thus inducing apoptosis in cancer cells. In certain studies, the use of cisplatin in combination with other metal chelators has shown improvement in the uptake of the anticancer drug. CisplatiN - Bio-X™ is part of our Bio-X™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Pan-tyrosine kinase inhibitor (VEGFR2, c-MET, RET, KIT); anti-neoplastic</p>

<p>Padsevonil is an investigational antiseizure medication, which is a synthetic pharmaceutical compound. It is derived from extensive medicinal chemistry research aiming to address complex seizure disorders resistant to conventional treatments. Padsevonil functions by exhibiting a dual mechanism of action. It binds to synaptic vesicle protein 2A (SV2A) with high affinity, similar to levetiracetam but with additional modulation of the benzodiazepine-sensitive gamma-aminobutyric acid-A (GABA-A) receptor. This combined activity potentiates its efficacy in stabilizing neuronal hyperactivity and dampening excitatory neurotransmission, providing a novel angle to tackle refractory seizures.</p>

<p>A potent and selective inhibitor of cell death-inducing kinase RIP2 (IC50 = 5 nM). Reduces release of pro-inflammatory cytokines. Inhibits production of TNF-α and IL-6 in intestinal explants from patients with Crohn's disease and ulcerative colitis.</p>

<p>Aprepitant is a neurokinin-1 receptor antagonist. It is an antiemetic which suppresses nausea and vomiting and has proven to be especially useful alongside cancer chemotherapy and as a tool in cancer-related studies. Aprepitant binds to the neurokinin-1 receptor in the brain, preventing it from binding to substance P. This prevents substance P from stimulating nerves in the vomiting center of the brain, reducing feelings of nausea and vomiting. Aprepitant has been shown to be effective against HIV infection, with no major side effects. The use of aprepitant for HIV therapy may be limited due to its ability to cause serious liver damage when taken with other drugs that are metabolized by cytochrome P450 enzymes.</p>

<p>Sparteine hydroiodide is the salt form of sparteine. This compound acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.</p>

<p>Amantadine is an antiviral drug that is used to treat dyskinesia in patients with Parkinson’s disease. This drug’s mechanism is not fully understood however it is said to aid in releasing dopamine from the nerve ending in brain cells. Amantadine is also an NDMA antagonist.</p>

<p>H1-receptor antagonist</p>

<p>Toceranib phosphate is a receptor tyrosine kinase inhibitor. Toceranib phosphate has been shown to be effective in the treatment of skin cancer and other types of cancer, including lung cancer and breast cancer. It is approved in the US as a treatment for canine mastocytoma (mast cell tumours).</p>

<p>Lacidipine is a lipophilic dihydropyridine calcium channel blocker that is used in the treatment of hypertension. This drug acts as an antihypertensive agent to dilate peripheral arteries and reduces blood pressure. Lacidipine blocks voltage-dependent L-type calcium channels.</p>

<p>Sn(IV) mesoporphyrin IX dichloride is a synthetic porphyrin derivative, which is a metalloporphyrin complex formed by the incorporation of tin into the porphyrin structure. This compound originates from the modification of mesoporphyrin IX, a naturally occurring tetrapyrrole, and is further functionalized with chloride ligands. The mode of action of Sn(IV) mesoporphyrin IX dichloride primarily involves the inhibition of heme oxygenase, an enzyme responsible for the catabolism of heme into biliverdin, carbon monoxide, and free iron. This inhibition results in the modulation of heme metabolism, which can have broad implications in various physiological and pathological processes.</p>

<p>Cyamemazine is a neuroleptic medication, which is a member of the phenothiazine class of compounds. It is synthesized from derivatives of phenothiazine, a group of agents primarily found in pharmaceuticals. The mode of action of cyamemazine involves antagonism at dopamine D2 receptors in the central nervous system. This inhibition of dopamine activity is the principal mechanism through which it exerts its antipsychotic effects. Due to its receptor activity, cyamemazine is used primarily in the management of various psychotic disorders, including schizophrenia and acute psychoses. It also exhibits anxiolytic properties, making it effective in treating anxiety associated with these conditions. By modulating neurotransmitter pathways, cyamemazine helps to alleviate symptoms such as hallucinations, delusions, and agitation, offering therapeutic benefit in complex neuropsychiatric cases. As an atypical antipsychotic, it provides an option for patients who may not respond adequately to other treatments. Although primarily used in a clinical setting, ongoing research continues to investigate potential wider applications and efficacy in treating other mental health issues.</p>

<p>A potent inhibitor of ubiquitin activating enzyme E1. Lowers ubiquitin conjugates in cells, thereby disrupting cell signalling, cell cycle progression and repair of DNA damage. Anti-tumor effects have been demonstrated in vitro and in vivo. TAK 243 has been used to study the biology of ubiquitins and its potential as anti-cancer therapy.</p>

<p>Agonist of alpha7 subtype of nural nicotinic acetylcholine receptor</p>

<p>Etoposide is a cytotoxic drug used in cancer chemotherapy. It inhibits DNA replication through inhibition of DNA topoisomerase II, thus catalysing cell cycle arrest and apoptosis. <br>Etoposide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Finasteride is an antiandrogenic drug that belongs to the group of 5-alpha reductase inhibitors, which are used for the treatment of benign prostatic hyperplasia and male pattern baldness. The conversion of testosterone to 5α-dihydrotestosterone (DHT) is blocked by type II 5α-reductase inhibition, which then results in significant increase in prostatic testosterone concentrations and minimal to moderate increases in serum and tissue DHT concentrations. A reduction in DHT concentration will cause a reduction in prostatic volume as DHT appears to be the main androgen responsible for stimulating prostatic growth.</p>

<p>Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.</p>

<p>Farnesyl pyrophosphate synthase inhibitor</p>

<p>Increases VEGF via heme oxygenase-1 modulation; anti-ulcer agent</p>

<p>Fondaparinux sodium is an anticoagulant, which is a synthetic pentasaccharide based on the antithrombin-binding sequence of heparin. As a meticulously engineered compound, it is derived by chemical synthesis. Its mode of action involves the selective inhibition of factor Xa, a critical enzyme in the coagulation cascade. By binding specifically to antithrombin III, it enhances the inactivation of factor Xa, thereby interrupting the pathway that leads to thrombin formation and ultimately preventing fibrin clot formation.</p>

<p>Rofecoxib is a non-steroidal anti-inflammatory drug that is used to treat osteoarthritis, acute pain and migraine attacks. This drug is also a COX-2 inhibitor. As a result, it reduces inflammation and pain.</p>

<p>Apo-D human is a glycosylated lipocalin protein, which is primarily derived from human plasma. It plays a pivotal role in the regulation of lipid-related metabolic processes due to its ability to bind and transport various ligands, including steroids and lipids. The protein's mode of action involves its function as a shuttle for small hydrophobic molecules, impacting cholesterol metabolism and potentially influencing lipid-related signaling pathways.</p>

<p>Inhibitor of metalloendopeptidase neprilysin</p>

<p>Beta-adrenoceptor antagonist; anti-hypertensive</p>

<p>Lofexidine is a drug that belongs to the group of α2-adrenergic receptor antagonists. It has been shown to reduce the symptoms of withdrawal from opiates and cocaine, as well as alcohol and nicotine. This drug inhibits the enzyme cAMP which catalyzes the conversion of dopamine to norepinephrine by preventing it from binding to its receptor site on cells.</p>

<p>Moexipril is an angiotensin converting enzyme inhibitor that is used for the treatment of hypertension. This drug is a prodrug for moexiprilat and works by relaxing the blood vessels causing them to widen and lowering blood pressure. Moexipril has been shown to be effective in treating metabolic disorders such as congestive heart failure.</p>

<p>Muscarinic antagonist; bronchodilator</p>

<p>Muscarinic acetylcholine receptor agonist</p>

<p>N-Desmethyl ibandronate sodium is a white crystalline solid with a melting point of 238-240 °C. It has versatile building block, complex compound and research chemicals applications. It is an intermediate used in the synthesis of other compounds, such as speciality chemicals, useful intermediates and useful scaffolds. N-Desmethyl ibandronate sodium can be used in reactions that require high quality and high purity products.</p>

<p>VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic</p>

<p>Induces expression of Oct3/4 transcription factor</p>

<p>Antagonist of dopamine (D2), serotonin (5-HT2A) and histamine H1 receptors</p>

<p>Lestaurtinib is a multitarget tyrosine kinase inhibitor of the JAK, FLT-3 and TrkA families of tyrosine kinases at nanomolar concentrations. It inhibits proliferation and induces apoptosis in vitro. Lestaurtinib is a FDA approved orphan drug for acute myeloid leukemia.</p>

<p>Inhibitor of vacuolar-type proton pump</p>

<p>Timolol is an ophthalmic beta-adrenergic blocker that is used to lower the intraocular pressure in patients with glaucoma. It is also used to treat hypertension, as well as other conditions, such as arrhythmias, thyrotoxicosis and angina pectoris. The drug acts by blocking β1-receptors on the surface of heart muscle cells and blood vessels, thereby reducing the workload on the heart and lowering blood pressure.</p>

<p>Thyrotropin-releasing hormone (TRH) receptor agonist; TRH analogue</p>

<p>Inhibitor of proteaseγ‐secretase, which allows to modulate of the activity of γ‐secretase substrates Notch, E-cadherin, ErbB4, and amyloid precursor protein (APP). The compound can inhibit the growth of tongue carcinoma cells by arresting cell cycle in G0–G1 phase, modulate the activity of Notch1 receptor and Caspase-3 protease and induce apoptosis. It was also demonstrated that this inhibitor reduces the levels of β-amyloid peptide in the brain of mice model for Alzheimer’s disease. This compound also enhances the neuronal differentiation embryonic cells.</p>

<p>Antagonist of platelet activating factor</p>

<p>Endothelin A receptor antagonist</p>

<p>A potent small-molecule activator of UNC-51-like kinase 1 (ULK1), a serine-threonine kinase involved in autophagy. Promotes cytoprotective autophagy in MPP+-treated SH-SY5Y cells, via the ULK complex. Improves motor dysfunction and reduces loss of dopaminergic neurons, mediated by MPTP, in in vivo models of Parkinson’s disease.</p>

<p>GnRH super-agonist</p>

<p>Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II.</p>

<p>Selective antagonist of the serotonin receptors 5-HT2A with subnanomolar affinity. The compound has clozapine-like anti-psychotic properties and more favourable CNS safety profile than traditional anti-psychotics. MDL 100907 has been used in studies on antisocial behaviour in mice and shown that the blockage of 5-HT2A receptors leads to decreased post-traumatic aggression and bradycardia.</p>

<p>Inhibitor of protein kinase CK1</p>

<p>Azilsartan is an angiotensin II receptor blocker that is used to treat hypertension. It blocks the binding of angiotensin II receptors to the AT1 receptor by selectively binding to AT1 receptors as an antagonist, blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.</p>

<p>Selective vasopressin receptor V2 agonist</p>