nampt

NAMPT Activator-1 (compound 1) is an effective and specific activator of niacinamide phosphotransferase (Compound 1) with a wide range of EC50 (3.3-3.7 μM). NAMPT activator-1 effectively protects cultured cells from FK866-mediated toxicity and is a potential neuroprotective compound.

Nampt activator-2 is a NAMPT activator (EC50: 0.023 μM). Nampt activator-2 has an affinity for CYP2C9, 2D6, and 2C19 with affinity values of 0.060 μM, 0.41 μM, and 0.59 μM, respectively.Nampt activator-2 can be used in the study of atherosclerosis, obesity, type II diabetes, insulin resistance, and type I diabetes.

Nampt-IN-5 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

LB-60-OF61 is a NAMPT inhibitor that exhibits antiproliferative activity against MYC oncogene-dependent cancer cell lines (brackets).

OT-82 is a potent, selective, and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

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

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

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

Daporinad hydrochloride (FK 866 hydrochloride) is a potent nicotinamide-phosphate ribosyltransferase (NAMPT) inhibitor with potential anti-tumor and anti-angiogenic activity that induces apoptosis in tumor cells.Daporinad hydrochloride can be used in the study of inflammation and cancer.

Teglarinad chloride (GMX-1777 chloride) is a potent inhibitor of NAMPT, the precursor of GMX1778.Teglarinad chloride has antitumor activity and acts by interfering with DNA repair and inhibiting angiogenesis.

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

KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

STF-118804, a highly specific NAMPT inhibitor, reduces the viability of most B-ALL cell lines with an IC50 of less than 10 nM.

Nampt-IN-13 TFA is a NAMPT inhibitor (patent WO2021013693A1) suitable for synthesising antibody-drug conjugates (ADCs).

Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively).

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

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

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.

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).

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.

NAMPTactivator-8 (Compound 278) is an activator of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of less than 0.5 μM. It activates NAMPT in U2OS cells with a cellular EC50 also below 0.5 μM.