Nampt (Nicotinamide phosphoribosyl transferase) has been reported to be a cytokine that promotes B cell maturation and inhibits neutrophil apoptosis. NAmPRTase catalyzes the condensation of nicotinamide with 5-phosphoribosyl-1-pyrophosphate to yield nicotinamide mononucleotide, one step in the biosynthesis of nicotinamide adenine dinucleotide. The protein is an adipokine that is localized to the bloodstream and has various functions, including the promotion of vascular smooth muscle cell maturation and inhibition of neutrophil apoptosis. It also activates insulin receptor and has insulin-mimetic effects, lowering blood glucose and improving insulin sensitivity. The protein is highly expressed in visceral fat and serum levels of the protein correlate with obesity.


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Nampt activator-3

NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity[1].

  • CAS Number: 2790481-63-7
  • MF: C19H20N2O3
  • MW: 324.37
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-7

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[1].

  • CAS Number: 1223378-42-4
  • MF: C20H21N5O3
  • MW: 379.41
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-10 TFA

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[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-8

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[1].

  • CAS Number: 2453183-75-8
  • MF: C36H35N3O4
  • MW: 573.68
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GMX1778

GMX1778(CHS-828) is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM.IC50 value: < 25 nM [1]Target: NAMPT inhibitorin vitro: The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by GMX1778 (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (GMX1778-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM GMX1778 [1]. GMX1778 increases intracellular ROS in cancer cells by elevating the superoxide level while decreasing the intracellular NAD(+) level. Notably, GMX1778 treatment does not induce ROS in normal cells. GMX1778-induced ROS can be diminished by adding nicotinic acid (NA) in a NA phosphoribosyltransferase 1 (NAPRT1)-dependent manner [2].in vivo: A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of GMX1777 at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. GMX1777 at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg GMX1777 reduced the mortality associated with toxic doses of GMX1777 [1].

  • CAS Number: 200484-11-3
  • MF: C19H22ClN5O
  • MW: 371.864
  • Catalog: Nampt
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 526.9±58.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 272.4±32.3 °C

P7C3

P7C3 is a NAMPT activator. P7C3 can enhance learning and memory in aged rats. Protects newborn neurons in the dentate gyrus by mitigating cell death. In vitro: Administration of active P7C3 chemicals to cells treated with doxorubicin, which induces NAD depletion, led to a rebound in intracellular levels of NAD and concomitant protection from doxorubicin-mediated toxicity. In vivo: P7C3 is orally bioavailable, crosses the blood-brain barrier, and is non-toxic at doses several fold higher than the efficacious dose.An easily administered pro-neurogenic compound. The administration of P7C3 is 10mg/ kg( IP) in rats. Administration of P7C3 to normal mice, as well as npas3-/- mice, enhance survival of neurons subsequent to their birth in the SGZ.

  • CAS Number: 301353-96-8
  • MF: C21H18Br2N2O
  • MW: 474.188
  • Catalog: Nampt
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 656.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 350.8±31.5 °C

LB-60-OF61 hydrochloride

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[1].

  • CAS Number: 742064-38-6
  • MF: C29H31ClN6O2
  • MW: 531.05
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

STF 118804

STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.IC50 value:Target: NAMPT inhibitorin vitro: improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. STF-118804 displays distinctive cytotoxicity by inducing apoptosis without causing a phase-specific cell cycle arrest. Over-expression of NAMPT rendered 293T cells more resistant to STF-118804 resulting in a higher IC50 (106 nM, 95% CI 74–151 nM) compared to control cells (17 nM, 95% CI 13–23 nM), further confirming that NAMPT protein levels dictate sensitivity to STF-118804 [1].in vivo: STF-118804 displayed high efficacy in a xenograft model of ALL. Mice treated with STF-118804 over a 20-day period survived an average of 34 days longer than vehicle-treated animals. During treatment, bioimaging showed regression of tumor followed by suppression of disease. STF-118804 was tolerated in the efficacious dose range, and the absence of adverse physical or pathological effects indicated that toxicity was not limiting in a 20-day study of mock transplanted mice [1].

  • CAS Number: 894187-61-2
  • MF: C25H23N3O4S
  • MW: 461.533
  • Catalog: Nampt
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CB 300919

CB 300919 is a water-soluble analogue of CB30865; has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.IC50 value:Target: Nampt

  • CAS Number: 289715-28-2
  • MF: C32H34ClN7O2
  • MW: 584.11100
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SBI-797812

SBI-797812 is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT with EC50 of 0.37 μM. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+[1].

  • CAS Number: 2237268-08-3
  • MF: C19H22N4O4S
  • MW: 402.47
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NAMPT inhibitor-linker 1

NAMPT inhibitor-linker 1 is a drug-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.

  • CAS Number: 2241019-57-6
  • MF: C36H37FN6O6
  • MW: 668.71
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt activator-2

Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM)[1].

  • CAS Number: 2237268-90-3
  • MF: C17H15ClN4O3S
  • MW: 390.84
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NAMPT inhibitor-linker 2

NAMPT inhibitor-linker 2 is a drug-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.

  • CAS Number: 2241014-82-2
  • MF: C34H33FN6O5
  • MW: 624.66
  • Catalog: Drug-Linker Conjugates for ADC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LB-60-OF61

LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Teglarinad chloride

Teglarinad chloride (GMX1777) is a prodrug 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[1][2].

  • CAS Number: 432037-57-5
  • MF: C30H43Cl2N5O8
  • MW: 672.59700
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 158-159ºC
  • Flash Point: N/A

Nampt-IN-9

Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research[1].

  • CAS Number: 2180973-35-5
  • MF: C26H33N3O4
  • MW: 451.56
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NAMPT/IDO1-IN-1

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[1].

  • CAS Number: 2247884-06-4
  • MF: C23H24BrFN8O3
  • MW: 559.39
  • Catalog: Indoleamine 2,3-Dioxygenase (IDO)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt activator-1

Nampt activator-1 (compound 1) is a potent Nicotinamide phosphoribosyltransferase (NAMPT) activator, with EC50 of 3.3-3.7 μM[1].

  • CAS Number: 701929-65-9
  • MF: C16H17N3O3
  • MW: 299.32
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CB30865

CB30865(ZM 242421) is a potent inhibitor of Nampt , an enzyme present in the NAD biosynthetic pathway. IC50 value:Target: NamptCancer cells develop dependence on Nampt due to increased energy requirements and the elevated activity of NAD consuming enzymes such as sirtuins and mono and poly(ADP-ribose) polymerases (PARPs). These findings suggest new chemical starting points for Nampt inhibitors and further implicate this enzyme as a target in cancer.

  • CAS Number: 206275-15-2
  • MF: C26H22BrN5O2
  • MW: 516.38900
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-617

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.

  • CAS Number: 1362154-70-8
  • MF: C21H15F2N3O3S
  • MW: 427.42400
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KPT-9274

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

  • CAS Number: 1643913-93-2
  • MF: C35H29F3N4O3
  • MW: 610.625
  • Catalog: PAK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 857.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 472.4±34.3 °C

GNE-618

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[1].

  • CAS Number: 1362151-42-5
  • MF: C21H15F3N4O3S
  • MW: 460.43
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-3

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[1].

  • CAS Number: 2121591-52-2
  • MF: C29H25N7O2
  • MW: 503.55
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-5

Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1].

  • CAS Number: 2380013-17-0
  • MF: C25H25N5O2
  • MW: 427.50
  • Catalog: Nampt
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GPP78

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[1][2].

  • CAS Number: 1202580-59-3
  • MF: C27H29N5O
  • MW: 439.552
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

OT-82

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[1].

  • CAS Number: 1800487-55-1
  • MF: C26H21FN4O
  • MW: 424.47
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nampt-IN-1

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

  • CAS Number: 1698878-14-6
  • MF: C20H25N3O5S
  • MW: 419.495
  • Catalog: Nampt
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 659.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 352.9±34.3 °C

FK866 (APO866, Daporinad)

FK866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with an IC50 of 0.09 nM.

  • CAS Number: 658084-64-1
  • MF: C24H29N3O2
  • MW: 391.506
  • Catalog: Autophagy
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 629.9±51.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 334.8±30.4 °C