Organometallic Ligands

<p>Aripiprazole is an antipsychotic drug that is used in the treatment for various mood and psychotic disorders such as schizophrenia, depression and bipolar disorder. Although, its mechanism is not fully understood, the antipsychotic action of aripiprazole is likely due to its partial agonist activity on D2 and 5-HT1A receptors as well as its antagonist activity at 5-HT2A receptors.</p>

<p>A selective inhibitor of MEK1/2 kinase. Anti-proliferative and pro-apoptotic in multiple myeloma (MM) cells via G0/G1 cell cycle arrest and caspase 3 and PARP cleavage, respectively. Synergistic with other anti-MM therapies. Has anti-tumor effects in some solid tumors, such as in K-ras mutated colorectal cancer.</p>

<p>A potent inhibitor of phosphodiesterase type 9 (PDE9) tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. Has therapeutic potential for Alzheimer’s disease.</p>

MK 886 is a leukotriene antagonist that has been studied for use in treating atherosclerosis. This drug inhibits the 5-lipoxygenase activating protein thus inhibiting 5-lipoxygenase.

<p>Anti-inflammatory; inducer of P450 II B family</p>

<p>Synthetic estradiol derivative</p>

<p>Allosteric activator of AMP-activated protein kinase (AMPK) acting on the AMPK-β subunit with therapeutic potential in metabolic disorders such as diabetes, obesity, etc. A769662 also blocks the differentiation of mouse embryonic stem cells (mESCs) and maintains the mESCs in naïve state even in the absence of leukemia inhibitory factor (2i/L).</p>

<p>Short acting monoamine oxidase inhibitor</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>

<p>Inhibitor of carbonic anhydrase; muscle relaxant</p>

<p>Fludarabine triphosphate trisodium is a nucleotide analog, which is a type of chemotherapy agent derived from purine nucleosides. This compound is the active metabolite of fludarabine, sourced from synthetic chemistry designed to mimic naturally occurring nucleotides involved in DNA replication. The mode of action involves its incorporation into the DNA strand during replication, where it effectively inhibits DNA polymerase and ribonucleotide reductase. This disruption impairs DNA synthesis, leading to apoptosis or programmed cell death, particularly in rapidly dividing cancer cells.</p>

<p>AZD9567 is a selective glucocorticoid receptor modulator (SGRM), which is a synthetic pharmaceutical compound. Its source is rooted in medicinal chemistry efforts to design ligands that selectively interact with glucocorticoid receptors. The mode of action of AZD9567 involves binding to glucocorticoid receptors with high specificity, modulating their activity to trigger anti-inflammatory and immunomodulatory responses while minimizing common side effects associated with traditional glucocorticoids.</p>

<p>Inhibits tankyrase (TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively), by binding to the catalytic poly-ADP-ribose polymerase (PARP) domain. This stabilizes cytoplasmic protein Axin, mediating β-catenin depletion and thereby suppresses Wnt signalling pathway. XAV 939 has anti-proliferative and pro-apoptotic effects on neuroblastoma and colorectal cancer cells.</p>

<p>5-HT3 receptor antagonist; alpha-7 nicotinic acetylcholine receptor partial agonist</p>

<p>Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.</p>

<p>Carvediol is a nonselective beta-adrenoceptor blocking agent and an alpha 1-adrenoceptor blocker. It can be used as a drug, belonging to the class of beta blockers, in the treatment of heart failure, coronary artery disease, and hypertension. Carvedilol has been shown to reduce the risk of death in patients with heart failure and improve symptoms. Furthermore it has an effect on blood pressure by decreasing peripheral vascular resistance and mean arterial pressure. Carvedilol can be metabolized by cytochrome P450 enzymes and CYP2D6 and CYP2C9 liver enzymes.</p>

<p>Loratadine is a non-sedating, inverse agonist antihistamine used for the treatment of allergic rhinitis, an IgE (immunoglobulin E) mediated disease. Loratadine binds to histamine H1 receptors, preventing histamine from binding and causing an allergic reaction.It has been found to inhibit the release of eosinophil cationic protein by acting on different components of allergic inflammation, in particular in the modulation of ICAM-1 expression on nasal epithelial cells as a mechanism of protective for the epithelium, and therefore, the damage of mucosa is reduced. In recent studies, it was found that loratadine is a potent HR1 antagonist with in vitro inhbitory effect on human mast-cell lines, HMC-1 (from mast cell leukaemia) with an IC50 between 10 and 50 μM.Loratadine 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 panPI3K/mTOR</p>

<p>Inhibitor of COX-2 and PDE4 enzymes; NSAID of coxib class</p>

<p>A potent non ATP-competitive inhibitor of MAP/ERK kinase (MEK). Has anti-tumor activity in melanoma and papillary thyroid cancer cells with B-Raf mutations. Enhances generation and survival of induced pluripotent stem cells (iPSCs).</p>