Nampt-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Nampt.html NAMPTNicotinamide phosphoribosyl transferase; PBEF; Visfatin; pre-B cell-enhancing factor; Pre-B cell colonyenhancing factorNicotinamide phosphoribosyltransferase (NAMPT) is the rate-limiting enzyme which catalyzes the conversion of nicotinamide(NAM)

2、 and phosphoribosyl-pyrophosphates to nicotinamide mononucleotide (NMN) in the mammalian nicotinamide adeninedinucleotide (NAD+) synthetic salvage pathway. NAMPT exists in two forms, intracellular NAMPT (iNAMPT) and extracellular NAMPT(eNAMPT).iNAMPT levels are high in brown adipose tissue (BAT), li

3、ver and kidney, intermediate in white adipose tissue (WAT), lung, spleen,testes and skeletal muscle, and undetectable in brain and pancreas. eNAMPT, thought to be produced through post-translationalmodification of iNAMPT, is released into plasma predominantly from adipose tissue, where it catalyses

4、the synthesis of NMN.Although intracellular NAMPT is a key enzyme in controlling NAD metabolism, eNAMPT has been reported to function as acytokine, with many roles in physiology and pathology. Circulating eNAMPT has been associated with several metabolic andinflammatory disorders, including cancer.w

5、ww.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Nampt.html NAMPT HYPERLINK https:/www.MedChemE/Targets/Nampt.html HYPERLINK https:/www.MedChemE/Targets/Nampt.html Inhibitors HYPERLINK https:/www.MedChemE/FK866.html (E)-Daporinad(FK866; APO866) Cat. No.: HY-50876 HYPERLINK https:/www.MedChemE/CB-

6、300919.html CB HYPERLINK https:/www.MedChemE/CB-300919.html HYPERLINK https:/www.MedChemE/CB-300919.html 300919Cat. No.: HY-14375(E)-Daporinad (FK866) is an effective inhibitor ofnicotinamide phosphoribosyltransferase(NMPRTase; Nampt) with an IC of 0.09 nM.50CB 300919 is a quinazoline-based antitumo

7、ur agentwith high activity in the CH1 human ovarian tumourxenograft. CB 300919 has a continuous exposure (96h) growth inhibition IC value of 2 nM in human50CH1 ovarian tumor xenograft.Purity: 99.94%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.53%Clinical Data: No Deve

8、lopment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/CB30865.html CB30865(ZM 242421) Cat. No.: HY-14373 HYPERLINK https:/www.MedChemE/GMX1778.html CHS-828(GMX1778) Cat. No.: HY-10079CB30865 (ZM 242421) is a nicotinamidephosphoribosyltransferase (Nampt) inhibitor,with po

9、tent cytotoxicity. CB30865 is highly potentagainst a variety of human tumour cell lines (IC50values in the 1-10 nM range).CHS-828 (GMX1778) is a competitive inhibitor ofnicotinamide phosphoribosyltransferase(NAMPT), with an IC less than 25 nM. CHS-82850(GMX1778) exerts a cytotoxic effect by decreasi

10、ngthe cellular level of NAD+ and exhibits a potentanticancer activity.Purity: 98.05%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.35%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/GNE-617.html GNE-617 HYPERLINK

11、https:/www.MedChemE/GNE-617.html HYPERLINK https:/www.MedChemE/GNE-617-hydrochloride.html GNE-617 HYPERLINK https:/www.MedChemE/GNE-617-hydrochloride.html HYPERLINK https:/www.MedChemE/GNE-617-hydrochloride.html hydrochlorideCat. No.: HY-15766 Cat. No.: HY-15766AGNE-617 is a specific NAMPT inhibitor

12、 thatinhibits the biochemical activity of NAMPT with anIC of 5 nM and exhibits efficacy in xenograft50models of cancer.GNE-617 hydrochloride is a specific NAMPTinhibitor that inhibits the biochemical activityof NAMPT with an IC of 5 nM and exhibits50efficacy in xenograft models of cancer.Purity: 99.

13、85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gne-618.html GNE-618 HYPERLINK https:/www.MedChemE/gne-618.html HYPERLINK ht

14、tps:/www.MedChemE/gpp78.html GPP78Cat. No.: HY-12628(CAY10618) Cat. No.: HY-14374GNE-618 is a potent, orally active nicotinamidephosphoribosyl transferase (NAMPT) inhibitorwith an IC of 6 nM. GNE-618 depletes NAD levels50and induces tumor cell death. Anti-tumor activity.GPP78 (CAY10618) is a potent

15、Nampt inhibitorwith an IC of 3.0 nM for50 nicotinamide adeninedinucleotide (NAD) depletion. GPP78 is cytotoxic toneuroblastoma cell line SH-SY5Y cells with an IC50of 3.8 nM by inducing autophagy. GPP78 hasanti-cancer and anti-inflammatory effects.Purity: 98.14%Clinical Data: No Development ReportedS

16、ize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 250 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 5 mg (11.38 mM * 1 mL in Methanol), HYPERLINK https:/www.MedChemE/lb-60-of61.html LB-60-OF61 HYPERLINK https:/www.MedChemE/lb-60-of61.html HYPERLINK https:/www.MedChemE/lb-60-of61-hydro

17、chloride.html LB-60-OF61 HYPERLINK https:/www.MedChemE/lb-60-of61-hydrochloride.html HYPERLINK https:/www.MedChemE/lb-60-of61-hydrochloride.html hydrochlorideCat. No.: HY-101280 Cat. No.: HY-101280ALB-60-OF61 is a NAMPT inhibitor and is acytotoxic compound with a selectivity towards MYCoverexpressin

18、g cell lines.LB-60-OF61 hydrochloride is a potent NAMPT(nicotinamide phosphoribosyltransferase)inhibitor. LB-60-OF61 hydrochloride is a cytotoxiccompound with a selectivity towards MYCoverexpressing cell lines.Purity: 99.25%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 m

19、gPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/NAMPT_inhibitor-linker_2.html NAMPT HYPERLINK https:/www.MedChemE/NAMPT_inhibitor-linker_2.html HYPERLINK https:/www.MedChemE/NAMPT_inhibitor-lin

20、ker_2.html inhibitor-linker HYPERLINK https:/www.MedChemE/NAMPT_inhibitor-linker_2.html HYPERLINK https:/www.MedChemE/NAMPT_inhibitor-linker_2.html 2Cat. No.: HY-112616 HYPERLINK https:/www.MedChemE/Nampt-IN-1.html Nampt-IN-1(LSN3154567) Cat. No.: HY-12971NAMPT inhibitor-linker 2 is a drug-linkercon

21、jugates for ADC, composed of an NAMPTinhibitor as a payload, and a linker.Nampt-IN-1 (LSN3154567) is a potent and selectiveNAMPT inhibitor. Nampt-IN-1 inhibits purifiedNAMPT with an IC of 3.1 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.48%Clinical Data: No Develo

22、pment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/nampt-in-3.html Nampt-IN-3 HYPERLINK https:/www.MedChemE/nampt-in-3.html HYPERLINK https:/www.MedChemE/nampt-in-5.html Nampt-IN-5Cat. No.: HY-108701 Cat. No.: HY-130606Nampt-IN-3 (Compound 35) simultaneously inhi

23、bitnicotinamide phosphoribosyltransferase (NAMPT)and HDAC with IC s of 31 nM and 55 nM,50respectively. Nampt-IN-3 effectively induces cellapoptosis and autophagy and ultimately leads tocell death.Nampt-IN-5 is a potent nicotinamidephosphoribosyltransferase (NAMPT) inhibitor.Nampt-IN-5 also inhibits

24、CYP3A4 activity and hascellular IC s of 0.7 nM and 3.9 nM against A278050and COR-L23, respectively.Purity: 99.27%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.21%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 1

25、00 mg HYPERLINK https:/www.MedChemE/ot-82.html OT-82 HYPERLINK https:/www.MedChemE/ot-82.html HYPERLINK https:/www.MedChemE/sbi-797812.html SBI-797812Cat. No.: HY-136241 Cat. No.: HY-126255OT-82 is a potent, selective and orally activeinhibitor of NAMPT. OT-82 is selectively toxicto cells of hematop

26、oietic origin and inducescell death in a NAD+ dependent manner. OT-82 is apromising antineoplastic agent for the study ofhematological malignancies.SBI-797812 is structurally similar to active-sitedirected NAMPT inhibitors and blocks binding ofthese inhibitors to NAMPT with EC of 0.37 M.50Purity: 99.84%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 1