NAMPT Inhibitor

GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC₅₀ values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD⁺ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.

NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC₅₀s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel.

PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC₅₀ values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).

Nampt-IN-21 is a NAMPT inhibitor. Nampt-IN-21 serves as a Ligand for Target Protein for PROTAC for the synthesis of PROTAC NAMPT degraders, such as PROTAC NAMPT Degrader-30 (HY-152154). Nampt-IN-21 is applicable to the research of ovarian cancer.

MS7 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). NAMPT is overexpressed in many cancer cells to meet the continuous replenishment of NAD⁺ required for rapid proliferation. MS7, as a NAMPT target protein ligand, can be used to synthesize PROTAC A7, which is an effective NAMPT degrader. MS7 can be used in cancer research.

Nampt-IN-7 (compound GF8) is a potent NAMPT inhibitor, with an IC₅₀ of 7.31 μM. Nampt-IN-7 also displays cytotoxic activity against human HepG2 hepatocellular carcinoma cell line with an IC₅₀ of 24.28 μM.

Daporinad (FK866) hydrochloride is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a K_i value of 0.3 nM. Daporinad hydrochloride depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad hydrochloride causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad hydrochloride induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad hydrochloride can be used for the study of myeloma, liver cancer, and immunosuppression.

Nampt-IN-10 trihydrochloride (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 trihydrochloride shows cellular potency to A2780 and CORL23 cell lines with IC₅₀ values of 5 and 19 nM, respectively. Nampt-IN-10 trihydrochloride can be used as a novel non-antimitotic payload for antibody-drug conjugate (ADC).

Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC₅₀ of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS.

NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC₅₀ of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency.

Nampt-IN-19 is an orally active and non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with a human K_i of 5.6 nM. Nampt-IN-19 blocks NAD⁺ biosynthesis from Nicotinamide (HY-B0150). Nampt-IN-19 acts as an antiproliferative agent in cancer cells. Nampt-IN-19 has preclinical pharmacokinetic properties supporting oral antitumor activity in mouse xenograft models. Nampt-IN-19 can be used for the research of colorectal cancer.

AS1604498 is a highly specific competitive inhibitor of human NAMPT, with an IC₅₀ of 44.4 nM. AS1604498 functionally inhibits NAMPT enzymatic activity, reduces nicotinamide mononucleotide production, decreases intracellular NAD levels, activates caspase 3/7 and induces cancer cell apoptosis. AS1604498 is applicable to research related to chronic myeloid leukemia.

PARP1/NAMPT-IN-2 (Compound 13j) is a dual PARP/NAMPT inhibitor with IC₅₀ values of 0.8 nM and 18 nM for PARP1 and NAMPT, respectively. PARP1/NAMPT-IN-2 can inhibit the proliferation, migration and induce apoptosis of breast cancer cells. PARP1/NAMPT-IN-2 can be used for the research of triple-negative breast cancer.

LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system.

SHP2/NAMPT-IN-1 is an orally active dual inhibitor of SHP2 and NAMPT, with IC₅₀ values of 30.5 nM and 24.4 nM, respectively. SHP2/NAMPT-IN-1 reduces NAD⁺ levels and p-ERK expression by inhibiting NAMPT. SHP2/NAMPT-IN-1 can inhibit the migration and colony formation of MDA-MB-231 cells and promote apoptosis. SHP2/NAMPT-IN-1 has anti-proliferative activity against a variety of tumor cell lines and can reverse PD-L1-mediated T-cell immunosuppression. SHP2/NAMPT-IN-1 can be used for breast cancer research.

Nampt-IN-18 (Compound Q24) is an orally active NAMPT inhibitor with an IC₅₀ of 8.0 nM against hNAMPT. Nampt-IN-18 inhibits NAMPT enzymatic activity. Nampt-IN-18 inhibits DNA synthesis and induces Apoptosis. Nampt-IN-18 exhibits anticancer activity against gastric cancer and colorectal cancer. Nampt-IN-18 can be used for the research of gastrointestinal cancers.

Nampt-IN-22 is a nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-22 blocks the NAD⁺ salvage synthesis pathway by inhibiting nicotinamide phosphoribosyltransferase (NAMPT). Its tertiary alcohol forms hydrogen bonds with His191 of NAMPT and enhances lysosomal stability via intramolecular hydrogen bonds. As an ADC payload, Nampt-IN-22 exhibits low nanomolar cytotoxicity against tumor cells after conjugation to an anti-CD30 antibody, prolongs survival in a disseminated L540 Hodgkin lymphoma mouse model, and suppresses subcutaneous tumor growth. Nampt-IN-22 can be used in studies related to Hodgkin lymphoma.

GNE-617 (Standard) is the analytical standard of GNE-617. This product is intended for research and analytical applications. GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.

CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC₅₀ less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD⁺ and exhibits a potent anticancer activity.

Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC₅₀ of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition.