CHS-828

AdipoGen Life Sciences
Product Code: AG-CR1-0064
CodeSizePrice
AG-CR1-0064-M0055 mg£70.00
Quantity:
AG-CR1-0064-M02525 mg£250.00
Quantity:
Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
-20°C
Storage:
-20°C

Images

1 / 1
Chemical Structure

Chemical Structure

Further Information

Alternate Names/Synonyms:
GMX1778; (E)-1-[6-(4-Chlorophenoxy)hexyl]-2-cyano-3-(pyridin-4-yl)guanidine
Appearance:
White to off-white solid.
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.
CAS:
200484-11-3
EClass:
32160000
Form (Short):
liquid
InChi:
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)
InChiKey:
BOIPLTNGIAPDBY-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 200484-11-3. Formula: C19H22ClN5O. MW: 371.9. Antitumor compound. Programmed cell death inducer. Cytotoxic. Antiproliferative. p53 activator. IkappaB kinase inhibitor. NF-kappaB inhibitor. Nampt/visfatin inhibitor.
MDL:
MFCD03700766
Molecular Formula:
C19H22ClN5O
Molecular Weight:
371.9
Package Type:
Vial
Product Description:
Antitumor compound [1, 2, 8]. Programmed cell death inducer [3-5]. Cytotoxic [6, 7, 14]. Antiproliferative [11]. p53 activator [9]. IkappaB kinase inhibitor [10]. NF-kappaB inhibitor [10, 12]. Nampt/visfatin inhibitor [13, 15, 16].
Purity:
>98% (HPLC & NMR)
SMILES:
ClC1=CC=C(OCCCCCCNC(NC2=CC=NC=C2)=N/C#N)C=C1
Solubility Chemicals:
Soluble in DMSO, 100% ethanol or dimethylformamide.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

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. L?vborg, 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. L?vborg, 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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