A Nampt inhibitor
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Pro-drug Form(s)
38798GMX1777
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CHS-828

Item No. 11021

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[6-(4-chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinyl-guanidine
CAS Number
200484-11-3
Synonyms
  • GMX 1778
Molecular Formula
C19H22ClN5O
Formula Weight
371.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 0.5 mg/ml
λmax
231, 258 nm
SMILES
N#CN/C(NCCCCCCOC1=CC=C(Cl)C=C1)=N\C2=CC=NC=C2
InChi Code
InChI=1S/C19H22ClN5O/c20-16-5-7-18(8-6-16)26-14-4-2-1-3-11-23-19(24-15-21)25-17-9-12-22-13-10-17/h5-10,12-13H,1-4,11,14H2,(H2,22,23,24,25)
InChi Key
BOIPLTNGIAPDBY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    CHS-828 is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor (IC50 = <25 nM).1 It selectively inhibits Nampt over nicotinamide/nicotinic acid mononucleotide adenylyltransferase 1 (NMN/NaMN adenylyltransferase 1) at 10 µM. CHS-828 (100 nM) reduces NAD+ levels in, and is cytotoxic to, HeLa cervical cancer cells. It decreases ATP levels in C666-1 nasopharyngeal and FaDu head and neck squamous cell carcinoma (HNSCC) cells in a time-dependent manner when used at concentrations of 10 and 20 nM, respectively.2 CHS-828 (100 and 250 mg/kg per week) reduces tumor growth in MCF-7 breast cancer and NYH small cell lung cancer mouse xenograft models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Watson, M., Roulston, A., Bélec, L., et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosythesis: Strategy for enhanced therapy in nicotinic acid phophoribosyltransferase 1-deficient tumors. Mol. Cell. Biol. 29(21), 5872-5888 (2009).

    2. Kato, H., Ito, E., Alajez, N.M., et al. Efficacy of combining GMX1777 with radiation therapy for human head and neck carcinoma. Clin. Cancer Res. 16(3), 898-911 (2010).

    3. Hjarnaa, P.J.V., Jonsson, E., Latini, S., et al. CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo. Cancer Res. 59(22), 5751-5757 (1999).