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

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

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

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

(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).

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 (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).

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.

BRD4/NAMPT-IN-1 (Compound A2) exhibits strong inhibitory effects on NAMPT and BRD4, with IC50 values of 35 nM (NAMPT) and 58 nM (BRD4). This compound significantly suppresses the growth and migration of liver cancer cells while promoting apoptosis. Additionally, BRD4/NAMPT-IN-1 demonstrates potent anticancer activity in HCCLM3 xenograft mouse models without noticeable toxicity.