NAMPT Inhibitor

Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a K_i value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad 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 induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression.

Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC₅₀s of <100 nM and 120 nM, respectively.

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

OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and?induces cell death in a NAD⁺ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.

L2-FK866 is an ADC payload-linker conjugate (Drug-linker conjugate for ADC). L2-FK866 contains the ADC linker (Val-Cit-p-aminobenzyl) and the NAMPT inhibitor FK866 (HY-50876). L2-FK866 can be conjugated with Dinutuximab (HY-P9933) to form an ADC. L2-FK866 is applicable to neuroblastoma research.

Nampt-IN-20 is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor with a IC₅₀ of 9.0 nM. Nampt-IN-20 binds to the active site of Nampt, occupies the NAM-binding region and disrupts NAD biosynthesis. Nampt-IN-20 exerts antiproliferative effects in A2780 ovarian cancer cells. Nampt-IN-20 can be used for the research of ovarian cancer.

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.

ALT-100 (Human IgG4) is a humanized antibody expressed in CHO, targeting NAMPT. ALT-100 (Human IgG4) consists of a huIgG1/huIgG4 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For inflammatory or fibrotic diseases, the isotype control for ALT-100 (Human IgG4) can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

ALT-100 (Human IgG1) is a humanized IgG1 monoclonal antibody that targets NAMPT. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

STF-118804 is a highly specific NAMPT inhibitor. STF-118804 activates AMPK and inhibits mTOR pathways. STF-118804 has antitumor activity against pancreatic cancer.

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

Nampt-IN-10 TFA (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 TFA shows cellular potency to A2780 and CORL23 cells lines with IC₅₀s of 5 and 19 nM, respectively. Nampt-IN-10 TFA can be used as a novel non-antimitotic payload for ADCs.

NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC₅₀s of <7 pM and 40 pM, respectively.

Nampt-IN-15 (Example 3) is an Nampt inhibitor. Nampt-IN-15 shows cytotoxicity against BxPC-3, HepG2, L540cy and MOLM-13, with IC₅₀s of 38.5 nM, 8 nM, 8.5 nM, 7 nM respectively.

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC₅₀ of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.

BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC₅₀=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects.

CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC₅₀ values in the 1-10 nM range). CB30865 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.

Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC₅₀s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.

GNE-617 hydrochloride 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.