Organometallic Ligands

Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit.

Candesartan is a drug that belongs to the class of angiotensin II receptor antagonists and is used to treat hypertension. It is used in combination therapy with other drugs, such as hydrochlorothiazide and amlodipine, to lower blood pressure. Candesartan inhibits the formation of angiotensin II, the receptor which causes vasoconstriction and increased blood pressure.

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.

Potent agonist of a1β1γ1 5′-adenosine monophosphate-activated protein kinase (AMPK). It binds to the allosteric drug and metabolite (ADaM) site at the α- and β- subunit interface of AMPK. It has potential for the treatment of diabetic nephropathy. PF 06409577 reduces infections caused by flaviviruses, mediated by changes in the metabolism of lipids in host cells.

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.

Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling

alpha-adrenoceptor agonist; nasal decongestant

Interleukin-13 human is a recombinant cytokine, which is derived from the expression of the human IL-13 gene in suitable host systems, such as E. coli or mammalian cells. This cytokine belongs to the interleukin family and plays a pivotal role in the immune response by modulating inflammatory pathways. The mode of action of interleukin-13 involves binding to specific cell surface receptors, IL-13Rα1 and IL-13Rα2, which facilitates the activation of various intracellular signaling cascades, including the JAK/STAT pathway. This promotes the differentiation and proliferation of certain immune cells, influencing the production of IgE and contributing to the regulation of inflammatory responses.

Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.

Histamine (H2) receptor antagonist

S26131 is an advanced glycation end product (AGE) inhibitor, which is a synthetic compound designed for laboratory research purposes. It is derived from chemical synthesis processes, offering a robust tool for investigating the biochemical pathways associated with glycation. Its mechanism of action involves the inhibition of AGE formation, which is a post-translational modification resulting from the non-enzymatic reaction between sugars and proteins or lipids. This biochemical modulation is vital for studying the implications of glycation in various physiological and pathological contexts.

Positive allosteric modulator of the metabotropic glutamate receptor mGluR5 with EC50 in submicromolar range. The compound is able to increase mGluR5 function in vitro and in vivo. A study showed that ADX-47273 enhanced fear extinction learning as well as improved reversal learning in experimental animals.

Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.

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.

Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).

Bosentan is a dual endothelin receptor antagonist that is used to treat hypertension. This drug works by blocking the action of endothelin molecules which prevents the narrowing of blood vessels and decreases blood pressure.

Inhibitor of p38 kinase