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.

Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.

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.

GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.

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.

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.

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.

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).

Angiotensin II receptor antagonist

Nilutamide is an antineoplastic agent that is used to treat prostate cancer. This drug is an androgen receptor antagonist and binds with androgen receptors thus blocking its action and resulting in growth arrest.