1. Metabolic Enzyme/Protease
  2. Nampt
  3. GNE-618

GNE-618 

Cat. No.: HY-12628
Handling Instructions

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.

For research use only. We do not sell to patients.

GNE-618 Chemical Structure

GNE-618 Chemical Structure

CAS No. : 1362151-42-5

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Description

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].

IC50 & Target

IC50: 6 nM (NAMPT)[1]

In Vitro

GNE-618 reduces levels of NAD with an EC50 of 2.6 nM in the NSCLC cell line Calu-6[1].
GNE-618 (10-30 nM; 72 hours) reveals an increase in the sub-2N population and a decreases in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells[1].
GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50 of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC50 of 25.8 ± 4.2 nM)[1]

In Vivo

GNE-618 (100 mg/kg; p.o.; twice daily for 5 days) significantly inhibits tumor growth by 88% and has minimal effects on body weight in STO#81 patient-derived gastric model[1].

Molecular Weight

460.43

Formula

C₂₁H₁₅F₃N₄O₃S

CAS No.

1362151-42-5

SMILES

O=C(NCC1=CC=C(S(=O)(C2=CC(C(F)(F)F)=CC=C2)=O)C=C1)C3=CC(C=NN4)=C4N=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GNE-618GNE618GNE 618NamptNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

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GNE-618
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HY-12628
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