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AdipoGen Life Sciences
CHS-828
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CHF 75.00
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AG-CR1-0064-M0055 mgCHF 75.00
AG-CR1-0064-M02525 mgCHF 300.00
Nampt (mouse) (rec.) (enzymatically active) (AG-40B-0179) is inhibited by the specific Nampt inhibitor CHS-828 (AG-CR1-0064).
Methods: The protein Nampt (mouse) (rec.) (1µM) is tested for activity in vitro using the Cyclex NAMPT Colorimetric Assay Kit (Cyclex / MBL, CY-1251) in the presence of different concentrations of CHS-828 (dissolved in DMSO). The IC50 of CHS-828 is 40nM in this experiment.
Methods: The protein Nampt (mouse) (rec.) (1µM) is tested for activity in vitro using the Cyclex NAMPT Colorimetric Assay Kit (Cyclex / MBL, CY-1251) in the presence of different concentrations of CHS-828 (dissolved in DMSO). The IC50 of CHS-828 is 40nM in this experiment.
| Product Details | |
|---|---|
| Synonyms | GMX1778; (E)-1-[6-(4-Chlorophenoxy)hexyl]-2-cyano-3-(pyridin-4-yl)guanidine |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H22ClN5O |
| MW | 371.9 |
| CAS | 200484-11-3 |
| Purity Chemicals | ≥98% (HPLC & NMR) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO, 100% ethanol or dimethylformamide. |
| Biological Activity |
Inhibits Nampt (Prod. No. AG-40B-0179) activity with an IC50 of 40nM (for 1µM of enzyme). CHS-828 was dissolved in DMSO. |
| InChi Key | BOIPLTNGIAPDBY-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(OCCCCCCN\C(NC2=CC=NC=C2)=N/C#N)C=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Antitumor compound [1, 2, 8].
- Programmed cell death inducer [3-5].
- Cytotoxic [6, 7, 14].
- Antiproliferative [11].
- p53 activator [9].
- IκB kinase inhibitor [10].
- NF-κB inhibitor [10, 12].
- Nampt/visfatin inhibitor [13, 15, 16].
Product References
- CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo: P.J. Hjarnaa, et al.; Cancer Res. 59, 5751 (1999)
- Novel cyanoguanidines with potent oral antitumour activity: C. Schou, et al.; Bioorg. Med. Chem. Lett. 24, 3095 (1997)
- Temporal effects of the novel antitumour pyridyl cyanoguanidine (CHS 828) on human lymphoma cells: P. Martinsson, et al.; Eur. J. Cancer 37, 260 (2001)
- Cyanoguanidine CHS 828 induces programmed cell death with apoptotic features in human breast cancer cells in vitro: C.M. Hansen, et al.; Anticancer Res. 20, 4211 (2000)
- Cell death with atypical features induced by the novel antitumoral drug CHS 828, in human U-937 GTB cells: P. Martinsson, et al.; Eur. J. Pharmacol. 417, 181 (2001)
- Model for time dependency of cytotoxic effect of CHS 828 in vitro suggests two different mechanisms of action: S.B. Hassan, et al.; J. Pharmacol. Exp. Ther. 299, 1140 (2001)
- Action of a novel anticancer agent, CHS 828, on mouse fibroblasts: increased sensitivity of cells lacking poly (ADP-Ribose) polymerase-1: H. Lövborg, et al.; Cancer Res. 62, 4206 (2002)
- A Phase I study of CHS 828 in patients with solid tumor malignancy: P. Hovstadius, et al.; Clin. Cancer Res. 8, 2843 (2002)
- Activation of p53 protein in normal and in tumor cells by a novel anticancer agent CHS 828: J. Wojciechowski, et al.; Drugs Exp. Clin. Res. 29, 53 (2003)
- Anticancer agent CHS 828 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity: L.S. Olsen, et al.; Int. J. Cancer 111, 198 (2004)
- Novel antiproliferative antitumor agents: M.M. Mader, et al.; Curr. Opin. Drug Discov. Devel. 8, 613 (2005)
- CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome: S.B. Hassan, et al.; Anticancer Res. 26, 4431 (2006)
- Anticancer agent CHS-828 inhibits cellular synthesis of NAD: U.H. Olesen, et al.; BBRC 367, 799 (2008)
- Structure-activity relationship analysis of cytotoxic cyanoguanidines: selection of CHS 828 as candidate drug: H. Lövborg, et al.; BMC Res. Notes 2, 114 (2009)
- The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors: M. Watson, et al.; Mol. Cell. Biol. 29, 5872 (2009)
- Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase: U.H. Olesen, et al.; BMC Cancer 10, 677 (2010)
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