NAMPT

CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM).

GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.

Nampt-IN-12 (compound 9), a derivative of N-Pyridinylthiophene carboxamid, exhibits activity against peripheral nerve sheath cancer cells. It is metabolized by the enzymes NAMPT and NMNAT1 within the NAD salvage pathway into an adenine dinucleotide (AD) derivative, an analog of NAD that can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) within the cells. Nampt-IN-12's effective blood-brain barrier permeability makes it suitable for research into cancers of the central and peripheral nervous system.

Nampt-IN-9 (Compound 8) is a potent inhibitor of NAMPT with anticancer properties.Nampt-IN-9 can be used to study ductal adenocarcinoma of the pancreas.

Teglarinad chloride (GMX-1777 chloride) is an inhibitor of NAMPT with antitumor activity that acts by interfering with DNA repair and inhibiting angiogenesis.

Nampt-IN-7 (GF8) inhibits NAMPT (IC50: 7.31 μM) and kills HepG2 cells (IC50: 24.28 μM).

A-1293201 is a potent and selective NAMPT inhibitor.

NAMPT activator-3: a NAT derivative, EC50 of 2.6 μM, KD 132 nM, protects cells, prevents FK866 toxicity, and is neuroprotective in CIPN mice.

Nampt activator-2: Potent NAMPT activator (EC50: 0.023 μM), binds CYP2C9 (0.060 μM), 2D6 (0.41 μM), 2C19 (0.59 μM); useful in metabolic disease research.

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).

Nampt-IN-10 TFA, a NAMPT inhibitor, shows potency in A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), suitable for ADC payloads.

LB-60-OF61 is a NAMPT inhibitor, a NAMPT inhibitor that displays antiproliferative activity against MYC oncogene-dependent cancer cell lines.

JGB-1-155, serving as a positive allosteric modulator (N-PAMs), effectively enhances the activity of nicotinamide phosphoribosyltransferase (NAMPT) with an EC 50 of 3.29 μM. It mitigates oxidative stress by elevating NAD+ levels in THP-1 human monocytes and reduces TNFα-induced reactive oxygen species (ROS) in HT-22 cells [1].

Nampt activator-4, a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT), has an EC50 of 0.058 μM and can enhance nicotinamide adenine dinucleotide (NAD+) levels in cells [1].

Nampt-IN-15 (Example 3) is a Nampt inhibitor that exhibits cytotoxic effects on various cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13. The respective IC50 values for these cell lines are 38.5 nM, 8 nM, 8.5 nM, and 7 nM.

PD-L1/Nampt-IN-1 is an orally active inhibitor that targets both PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase), with IC50 values of 63 nM and 582 nM, respectively. It exhibits cross-species affinity, with KD values of 52.6 nM for hPD-L1 and 49.1 nM for mPD-L1. This compound effectively suppresses tumor growth by activating the tumor immune microenvironment and is applicable in melanoma research.

Nampt-IN-14 (example 3) is an effective NAMPT inhibitor with an IC50 of 0.2 nM, suited for use in the synthesis of antibody-drug conjugates (ADCs).

Nampt-IN-13 (example 58m) is an NAMPT inhibitor used in the synthesis of antibody-drug conjugates (ADCs).

CB30865 (ZM 242421) is a selective and highly effective nicotinamide phosphoribosyltransferase (Nampt) inhibitor with potential antitumor activity.

NAMPT activator-6, a regulatory molecule for the optical control system of NAMPT and NAD+, can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) for light-dependent, reversible regulation of NAMPT and NAD+, thereby reducing toxicity associated with inhibitor-based PS-PROTACs. This enables antitumor activity and in vivo modulation of NAMPT and NAD+ through optical manipulation [1].