cd38 inhibitor 1

CD38 inhibitor 1 is a potent CD38 inhibitor that is effective against human CD38 (IC50 value is 7.3 nM) and mouse CD38 (IC50 value is 1.9 nM).

Ara-F-NAD+ sodium, an arabino analogue of NAD+, serves as a potent, reversible, and slow-binding inhibitor of the CD38 NADase [1] [2].

CD38 Inhibitor 3 (compound 1), with an IC50 of 11 nM, is a potent agent that enhances mitochondrial biogenesis, diminishes lactate levels, and augments both NAD+ content and Nrf2 expression. In a Pus1 - - mouse model of mitochondrial myopathy, it also elevates muscle function and bolstering exercise capacity [1].

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38. At a concentration of 1 mM, it effectively inhibits the rise in intracellular calcium levels and chemotaxis triggered by N-formyl-Met-Leu-Phe (fMLP) in mouse bone marrow-derived neutrophils. Furthermore, when applied at 100 µM, this compound reduces LPS-induced nitrite production and decreases the secretion of TNF-α and IL-2 in mouse primary microglial cells.