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NAMPT Inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50876
    Daporinad
    Maximum Cited Publications
    64 Publications Verification

    FK866; APO866

    		 NAMPT Autophagy Apoptosis mTOR p38 MAPK ERK Cancer
    Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki 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 .
    Daporinad
  • HY-147193
    Nampt-IN-10 TFA

    		NAMPT Cancer
    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-IN-10 TFA
  • HY-136241
    OT-82
    1 Publications Verification

    		 NAMPT Caspase Cancer
    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 .
    OT-82
  • HY-12793
    Padnarsertib
    3 Publications Verification

    KPT-9274

    		 PAK NAMPT Cancer
    Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively .
    Padnarsertib
  • HY-18728
    STF-31
    15+ Cited Publications

    		 GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1 μM. STF-31 is also a NAMPT inhibitor. STF-31 inhibits glucose uptake in renal cell carcinoma (RCC) 4 cells .
    STF-31
  • HY-10079
    CHS-828
    4 Publications Verification

    GMX1778

    		 NAMPT Apoptosis Cancer
    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 .
    CHS-828
  • HY-15766
    GNE-617
    5+ Cited Publications

    		 NAMPT Metabolic Disease 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.
    GNE-617
  • HY-112615
    NAMPT inhibitor-linker 1

    		Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
    NAMPT inhibitor-linker 1
  • HY-402237
    Nampt-IN-15

    		NAMPT Neurological Disease Cancer
    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 .
    Nampt-IN-15
  • HY-12808
    STF-118804
    2 Publications Verification

    		 NAMPT AMPK mTOR Cancer
    STF-118804 is a highly specific NAMPT inhibitor. STF-118804 activates AMPK and inhibits mTOR pathways. STF-118804 has antitumor activity against pancreatic cancer .
    STF-118804
  • HY-112616
    NAMPT inhibitor-linker 2

    		NAMPT Drug-Linker Conjugates for ADC Cancer
    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 inhibitor-linker 2
  • HY-12971
    Nampt-IN-1
    2 Publications Verification

    LSN3154567

    		 NAMPT 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-1
  • HY-12628
    GNE-618
    2 Publications Verification

    		 NAMPT Cancer
    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 .
    GNE-618
  • HY-14373
    CB30865

    ZM 242421

    		 NAMPT Cancer
    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.
    CB30865
  • HY-N3225
    Myricanol

    		NAMPT Sirtuin Microtubule/Tubulin Apoptosis Autophagy PDGFR NF-κB AMPK Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation .
    Myricanol
  • HY-W017463
    trans-3-(3-Pyridyl)acrylic acid

    		Drug Intermediate TMV Isocitrate Dehydrogenase (IDH) Infection
    trans-3-(3-Pyridyl) acrylic acid is an unsaturated carboxylic acid and synthetic building block, which serves as a synthetic precursor of 3-(3-pyridyl) propanoic acid. trans-3-(3-Pyridyl) acrylic acid can be used to prepare dual mutant IDH1/NAMPT inhibitors and PGE2 antagonist analogs. In addition, trans-3-(3-Pyridyl) acrylic acid exhibits antiviral activity against tobacco mosaic virus (TMV) .
    trans-3-(3-Pyridyl)acrylic acid
  • HY-14374
    GPP78

    CAY10618

    		 NAMPT Autophagy Inflammation/Immunology Cancer
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects .
    GPP78
  • HY-108701
    Nampt-IN-3

    		NAMPT HDAC Autophagy Apoptosis Cancer
    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 .
    Nampt-IN-3
  • HY-10080
    Teglarinad chloride

    GMX1777; EB-1627

    		 NAMPT Cancer
    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 .
    Teglarinad chloride
  • HY-33287
    2-Bromothiazole-5-carboxylic acid

    		Biochemical Assay Reagents Cancer
    2-Bromothiazole-5-carboxylic acid is a starting compound in the synthesis of active compounds. 2-Bromothiazole-5-carboxylic acid can be used in the synthesis of NAMPT/HDAC inhibitors. 2-Bromothiazole-5-carboxylic acid can be used in the research of colon cancer, lung cancer, and liver cancer .
    2-Bromothiazole-5-carboxylic acid
  • HY-125147
    A-1293201

    		NAMPT Cancer
    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) .
    A-1293201
  • HY-155506
    NAMPT degrader-3

    		NAMPT Cancer
    NAMPT degrader-3 (compound C5) is a NAMPT degrader, depending on VHL- and proteasome manner. NAMPT degrader-3 displays cytotoxicity and inhibits A2780 cells proliferation .
    NAMPT degrader-3
  • HY-163445
    NAMPT activator-6

    		NAMPT Cancer
    NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
    NAMPT activator-6
  • HY-147193A
    Nampt-IN-10 trihydrochloride

    		NAMPT Cancer
    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-10 trihydrochloride
  • HY-161712
    IMPDH-IN-4

    		IMPDH Cancer
    IMPDH-IN-4 is a derivative of N-pyridinylthiophene carboxamid that exhibits activity against peripheral nerve sheath carcinoma cells. IMPDH-IN-4 is metabolized by NAMPT and NMNAT1 to an adenine dinucleotide (AD) derivative, which is an NAD analog and can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) in cells. IMPDH-IN-4 has good blood-brain barrier permeability and can be used in the study of central and peripheral nervous system cancers .
    IMPDH-IN-4
  • HY-164759
    Nampt-IN-13

    		NAMPT Cancer
    Nampt-IN-13 (example 58m) is a NAMPT inhibitor that can be used in the synthesis of Antibody-drug Conjugate (ADC) .
    Nampt-IN-13
  • HY-W1117786
    Nampt-IN-10

    		ADC Payload NAMPT Cancer
    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 .
    Nampt-IN-10
  • HY-15766A
    GNE-617 hydrochloride
    5+ Cited Publications

    		 NAMPT Cancer
    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.
    GNE-617 hydrochloride
  • HY-159009
    MS7

    		NAMPT Ligands for Target Protein for PROTAC 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 .
    MS7
  • HY-147838
    Nampt-IN-9

    		NAMPT Cancer
    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-9
  • HY-176237
    Nampt-IN-16

    		NAMPT Apoptosis Cancer
    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 .
    Nampt-IN-16
  • HY-170972
    PARP1/NAMPT-IN-2

    		Apoptosis PARP NAMPT Cancer
    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 .
    PARP1/NAMPT-IN-2
  • HY-130606
    Nampt-IN-5

    		NAMPT Cytochrome P450 Cancer
    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 .
    Nampt-IN-5
  • HY-162124
    HDAC/NAMPT-IN-1

    		NAMPT HDAC Cancer
    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 .
    HDAC/NAMPT-IN-1
  • HY-161515
    BRD4/NAMPT-IN-1

    		NAMPT Epigenetic Reader Domain Cancer
    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 .
    BRD4/NAMPT-IN-1
  • HY-175294
    PD-L1/Nampt-IN-1

    		PD-1/PD-L1 NAMPT 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 KD 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 .
    PD-L1/Nampt-IN-1
  • HY-15766R
    GNE-617 (Standard)

    		NAMPT Metabolic Disease Cancer
    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.
    GNE-617 (Standard)
  • HY-148572
    NAMPT/IDO1-IN-1

    		Indoleamine 2,3-Dioxygenase (IDO) NAMPT Cancer
    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 .
    NAMPT/IDO1-IN-1
  • HY-162519
    LZFPN-90

    LZ90

    		 NAMPT PD-1/PD-L1 Apoptosis Metabolic Disease Inflammation/Immunology 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 .
    LZFPN-90
  • HY-162537
    LYP-8

    		PROTACs NAMPT Cancer
    LYP-8 is a potent and effective NAMPT degrader with maximum degradation of 97% at 0.5 μM in SKOV-3 cells. LYP-8 shows anti-cancer activity in vivo and in vitro(Sturcture Note:(Blue: Cereblon ligand (HY-112078), Black: linker (HY-128801)；Pink: Nampt inhibitor Nampt-IN-11 (HY-158689)) .
    LYP-8
  • HY-172919
    PDEδ/NAMPT IN-1

    		Phosphodiesterase (PDE) NAMPT Apoptosis Cancer
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=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 .
    PDEδ/NAMPT IN-1
  • HY-110319
    (E/Z)-Daporinad hydrochloride

    (E/Z)-FK866 hydrochloride; (E/Z)-APO866 hydrochloride

    		 NAMPT Apoptosis Inflammation/Immunology Cancer
    (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 .
    (E/Z)-Daporinad hydrochloride
  • HY-161180
    Antitumor agent-136

    		NAMPT Cancer
    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 .
    Antitumor agent-136
  • HY-164705
    Mal-Toxophore

    		Drug-Linker Conjugates for ADC Cancer
    Mal-Toxophore is a drug-linker conjugate for ADC and can be used for ADC synthesis. The payload is a NAMPT inhibitor (HY-164759) .
    Mal-Toxophore
  • HY-161051
    Anticancer agent 177

    		NAMPT DNA Alkylator/Crosslinker Cancer
    Anticancer agent 177 (Compound 11b) is a NAMPT inhibitor and DNA alkylating agent. Anticancer agent 177 has antitumor activity in vitro and in vivo .
    Anticancer agent 177
  • HY-147795
    Nampt-IN-8

    		Quinone Reductase NAMPT Apoptosis Reactive Oxygen Species (ROS) Cancer
    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-IN-8
  • HY-147756
    Nampt-IN-7

    		NAMPT Cancer
    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 .
    Nampt-IN-7
  • HY-158319
    Mutant IDH1/NAMPT-IN-1

    		Apoptosis Isocitrate Dehydrogenase (IDH) NAMPT Cancer
    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 .
    Mutant IDH1/NAMPT-IN-1
  • HY-159015
    SIAIS630120-NC

    		PROTACs Cancer
    SIAIS630120-NC is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) degrader SIAIS630120 (Sturcture Note:(Blue: Cereblon ligand Thalidomide (HY-14658) analogue (HY-138793), Black: linker；Pink: Nampt inhibitor FK866 (HY-50876)) .
    SIAIS630120-NC
  • HY-101280
    LB-60-OF61

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

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