T6146

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

Tyrosinase-IN-3 (compound 54) is a potent inhibitor of tyrosinase, a copper-containing metalloenzyme essential in melanin biosynthesis and enzymatic browning, showing potential for research in skin whitening agents and food preservatives [1].

Anticancer agent 37 (compound 18) is a sulfonylurea derivative known for its potent anticancer activity. It efficiently inhibits the growth of HePG2 cells, displaying an IC 50 value of 17.2 μg/mL [1].

EV-A71-IN-1 is a potent inhibitor of the human enterovirus A71 (EV-A71) capsid protein, with an EC50 of 0.27 μM against EV-A71. Acting as a capsid binder, EV-A71-IN-1 disrupts the crucial interaction between the viral VP1 protein and the host receptor hSCARB2. It displays broad-spectrum antiviral activity against various human enteroviruses, while being non-toxic to human cells (CC50 > 56.2 μM) [1].

Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a potent dual inhibitor of monoamine oxidase (MAO) and aromatase, with IC50 values of 39 nM for MAO-B and 31 nM for aromatase. It holds significant potential for research in neurological disorders and breast cancer [1].

TRβ agonist 2 (Compound 1) is a highly potent TRβ agonist that effectively reduces lipid accumulation in HepG2 cells and promotes lipolysis, offering comparable effects. With its promising attributes, TRβ agonist 2 emerges as a potential thyromimetic selectively targeting TRβ [1].

PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1].

PptT-IN-3 (compound 5p) is a powerful inhibitor (IC50 = 3.5 μM) of phosphopantetheinyl phosphoryl transferase (PptT), an indispensable enzyme involved in the synthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. This compound holds promise for tuberculosis research [1].

Esomeprazole magnesium salt is a potent and orally active proton pump inhibitor that effectively reduces acid secretion in gastric parietal cells by inhibiting the H+, K+-ATPase. This compound has shown promise for the research and treatment of symptomatic gastroesophageal reflux disease [1][2][3].

RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that disrupts the RAD51 BRCA2 protein-protein interaction in the micromolar range. This protein-protein interaction (PPI) inhibitor also demonstrates inhibitory activity for H4A4 with an EC50 value of 19 μM [1].