NAMPT Inhibitor

Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC₅₀s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.

LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.

CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC₅₀ value of 2 nM in human CH1 ovarian tumor xenograft. CB 300919 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD⁺/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079).

LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.

Anticancer agent 177 (Compound 11b) is a NAMPT inhibitor and DNA alkylating agent. Anticancer agent 177 has antitumor activity in vitro and in vivo.

(E/Z)-Daporinad hydrochloride ((E/Z)-FK866 hydrochloride) is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). (E/Z)-Daporinad hydrochloride induces apoptosis by specifically inhibiting NAMPT to gradually deplete intracellular NAD⁺. (E/Z)-Daporinad hydrochloride can be used in the study of cancer biology and inflammatory diseases.

Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity.

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (K_D=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC₅₀=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD⁺), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.

PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC₅₀s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable K_D values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma.

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-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma 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.

CAIX/XII/NAMPT-IN-1 is a triple inhibitor of carbonic anhydrase IX/XII and nicotinamide phosphoribosyltransferase (NAMPT) with a hCA IX K_i of 78.1 nM, hCA XII K_i of 64.4 nM, and hNAMPT IC₅₀ of 168 nM. CAIX/XII/NAMPT-IN-1 induces apoptosis, ROS accumulation, suppresses ERK/AKT signaling, inhibits DNA synthesis, and causes mitochondrial dysfunction. CAIX/XII/NAMPT-IN-1 exerts antiproliferative effects against multiple cancer cells under normoxic and hypoxic conditions. CAIX/XII/NAMPT-IN-1 can be used for the research of cancer, such as renal carcinoma, glioblastoma and colorectal cancer.

Gibberellin A34 is a Hypoxanthine guanine phosphoribosyltransferase 1 (HPRT1) inhibitor that can be isolated from immature seeds of Calonyction aculeatum. Gibberellin A34 can be used for studies on plant growth and development regulation.

Nampt-IN-13 is a NAMPT inhibitor that serves as a payload for the synthesis of ADCs. Nampt-IN-13 is applicable to cancer-related research.

HDAC/NAMPT-IN-1 (compound 39h) is a dual inhibitor of HDAC and NAMPT with IC₅₀ values of 0.72-37081 nM and 1618 nM.

Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC₅₀=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC₅₀=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively.

Nampt-IN-16 (Compound 9a) is an orally active NAMPT inhibitor with an IC₅₀ of 0.15 μM. Nampt-IN-16 can reduce intracellular NAD⁺ and ATP levels. Nampt-IN-16 can inhibit the proliferation, migration, and invasion, induce cell cycle arrest and apoptosis, and alter cellular metabolism of gastric cancer cells. Nampt-IN-16 can be used in the research of tumors such as gastric cancer.

TT-03597 is a modified NAMPT inhibitor core derived from OT-82 (HY-136241), which serves as a target protein ligand for PROTACs targeting NAMPT. TT-03597 can be used for the synthesis of PROTAC NAMPT Degrader-31 (HY-187347).