Activators & Inhibitors

Dazolicin HCl (Dazolicine HCl) is an orally available antiarrhythmic compound.

Delequamine (RS 15385-197) is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

RS 15385-198 is a less active isomer of Delequamine. Delequamine is a selective alpha2-adrenergic receptor antagonist.

Nufenoxole is an orally active and antidiarrhoeal compound that inhibits fluid secretion in the human jejunum.

Sanfetrinem (GV104326) sodium is a novel orally available β-lactamase antibiotic that shows significant antibacterial activity against Gram-positive and Gram-negative bacteria and can be used in the study of bacterial infections.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

OTUB1/USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1/USP8-IN-1 may be used in the study of leukaemia.

Canakinumab (ACZ885) is a recombinant human IL-1β-targeting monoclonal antibody.Canakinumab has been shown to inhibit human and chorioallantoic monkey IL-1β, with IC50 values of 43.6 and 40.8 pM, respectively.Canakinumab has anti-inflammatory activity, inhibiting inflammation associated with autoimmune diseases by neutralizing IL-1β signaling. Canakinumab has anti-inflammatory activity, inhibiting inflammation associated with autoimmune diseases by neutralizing IL-1β signaling.Canakinumab has been used for the treatment of gout and coronary artery disease.

Sonrotoclax is a potent, orally active inhibitor of Bcl2, demonstrating effective cell-killing activity against a range of lymphoma and leukemia cell lines [1].