CHS-828 (GMX-1778)

SKU: orb1306792

Description

CHS-828 (GMX1778) is a potent small molecule NAMPT inhibitor with an IC50 below 25 nM, disrupting cellular NAD+ biosynthesis. It is a valuable research tool for studying cancer metabolism and has demonstrated antitumor efficacy in both cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Epigenetics & Chromatin, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 200484-11-3
• MW: 371.86
• Purity: >98%
• Formula: C₁₉H₂₂ClN₅O
• SMILES: Clc1ccc(OCCCCCCNC(NC#N)=Nc2ccncc2)cc1
• Target: Energy production
• Solubility: Soluble in DMSO up to 25 mg/ml)

Bioactivity

• Target IC50:
  NAMPT:<25 nM
• In Vivo:
  GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice.
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• In Vitro:
  GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. GMX1778 induces programmed cell death with apoptotic features. GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM).
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• Cell Research:
  Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GMX-1778

Compound Identifiers

PubChem CID

148198