Organometallic Ligands

Ruxolitinib is a janus tyrosine kinase inhibitor active specifically on sub-types JAK1 and JAK2 with IC50 values in the nanomolar range. JAK1 and JAK2 are kinases involved in the regulation of hematopoiesis. Clinically applied to the treatment of intermediate and high-risk myelofibrosis, ruxolitinib is usually well tolerated by patients.

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.

PI3K/mTOR kinase inhibitor; anti-neoplastic

Inhibitor of FGFR kinase

Inhibitor of CETP exchange protein

Aurora kinase inhibitor

Antagonist of H1 histamine receptors

Inhibitor of cathepsins and other cysteine proteases

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.

Nicorandil is an ATP-dependent potassium channel activator. It activates mitochondrial ATP-dependent potassium (KATP) channels and inhibits the TLR4/MyD88/NF-κB/NLRP3 pathway, which reduces myocardial infarction-induced pyroptosis. Pyroptosis is an inflammatory cell death process that regulates cardiomyocyte loss after myocardial infarction. These findings suggest that nicorandil may be a potential therapy for ischemic heart disease due to its cardioprotective effects.

Inhibitor of the histone methyltransferase SETD8 that supresses methylation of the K20 residue in histone 4. UNC 0379 treatment of human glioma reduced recruitment of 53BP1 protein to double strand breaks and sensitised cells to radiotherapy without altering cell cycle kinetics.

Synthetic analog of vasopressin; anti-diuretic; hemostatic

Inhibitor of EGFR receptor

A potent antagonist of H2-receptor. Demonstrated effective and prolonged inhibition of gastric acid secretion after a single 100 mg or 200 mg dose in humans. Considered as a potential treatment for duodenal ulcer but incidences of idiosyncratic hepatocellular injury halted further development.

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.

Inhibits RGS proteins, selective for RGS4