NAMPT

MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), which is often overexpressed in cancer cells to sustain NAD+ levels necessary for rapid cell proliferation. By targeting NAMPT, MS7 serves as a valuable tool for developing PROTAC A7, an effective degrader of NAMPT. This reagent holds significant potential for research applications in cancer biology, particularly in studies focused on metabolic regulation and therapeutic strategies targeting NAMPT.

Nampt-IN-7 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis by targeting NAMPT, with an IC50 of 7.31 μM. This compound exhibits significant cytotoxicity against the HepG2 hepatocellular carcinoma cell line, demonstrated by an IC50 of 24.28 μM. Nampt-IN-7 is valuable for research applications focusing on cancer metabolism and therapeutic strategies targeting NAD+ synthesis in tumor cells.

NAMPT activator-6 is a potent activator of nicotinamide adenine monophosphate (NAMPT), playing a crucial role in the regulation of NAD+ biosynthesis. This compound facilitates reversible control over NAMPT and NAD+ levels through light-mediated techniques, enabling the development of photoswitchable proteolysis-targeting chimeras (PS-PROTACs). Research applications include modulation of NAMPT and NAD+ in vivo, offering potential for enhanced antitumor activity while minimizing the side effects associated with traditional inhibitors.

AS1604498 is a selective competitive inhibitor of human nicotinamide adenine dinucleotide (NAD) biosynthesis enzyme NAMPT, demonstrating an IC50 of 44.4 nM. By inhibiting NAMPT activity, AS1604498 effectively reduces the production of nicotinamide mononucleotide and lowers intracellular NAD levels, leading to the activation of caspase 3/7 and the subsequent induction of apoptosis in cancer cells. This compound is particularly relevant for research focused on chronic myeloid leukemia and related metabolic pathways.

NAMPT activator-8 is a potent activator of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of less than 0.5 μM. This compound effectively enhances NAMPT activity in U2OS cells, facilitating increased NAD+ synthesis. NAMPT activator-8 is valuable for research applications focused on metabolic regulation and cellular energy homeostasis.

Nampt-IN-17 is a selective inhibitor of nicotinamide adenine dinucleotide (NAD+) biosynthesis, targeting NAMPT with an IC50 of 17 nM and a Ki of 25.9 nM in human cells. This compound effectively depletes intracellular NAD+ and ATP levels, leading to disrupted mitochondrial membrane potential and subsequently inhibiting cell proliferation, self-renewal, invasion, and migration. Additionally, Nampt-IN-17 induces cell cycle arrest and apoptosis, demonstrating potent selectivity against NAPRT-deficient gastric cancer cells. It serves as a valuable tool for studying the mechanisms underlying NAPRT-deficient gastric cancer.