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044664 CHS-828 CAS: 200484-11-3

Specifications
References
CAS Number
200484-11-3
Grade
Highly Purified
MDL Number
MFCD03700766
Molecular Formula
C19H22ClN5O
Molecular Weight
371.9
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C/-20°C
GMX1778, (E)-1--2-cyano-3-(pyridin-4-yl)guanidine

Antitumor compound. Programmed cell death inducer. Cytotoxic. Antiproliferative. p53 activator. IkappaB kinase inhibitor. NF-kappaB inhibitor. Nampt/visfatin inhibitor.

Synonyms
GMX1778; (E)-1-[6-(4-Chlorophenoxy)hexyl]-2-cyano-3-(pyridin-4-yl)guanidine
CAS Number
200484-11-3
Molecular Weight
371.9
Molecular Formula
C19H22ClN5O
Solubility
DMSO, 100% ethanol or dimethylformamide
Biological Activity
Inhibits Nampt activity with an IC50 of 40nM (for 1uM of enzyme). 044664 was dissolved in DMSO.
Appearance
Supplied as a white to off-white solid.
Purity
≥98% (HPLC & NMR)
Storage and Stability
Store at 4°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards
 All products should be handled by qualified personnel only, trained in laboratory procedures.
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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