CHS828 Inhibitor CAS No. 200484-11-3

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Chemical Characteristic

Product Name	CHS828
CAS No.	200484-11-3
Molecular Weight	371.86
Formula	C₁₉H₂₂ClN₅O
Chemical Name	N-[6-(4-Chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinylguanidine;1-(6-(4-chlorophenoxy)hexyl)-2-cyano-3-(pyridin-4-yl)guanidine
Smiles	N(/C(=N/c1ccncc1)/NC#N)CCCCCCOc1ccc(cc1)Cl
Chemical Structure

Biological activities

CHS-828 is a competitive inhibitor of NAMPT and an inhibitor of NF-ΚB pathway activity as well, with anti-tumor activity in vitro and in vivo. The IKK activity is inhibited by CHS-828 with an IC(50) of 8 nM. In vitro, CHS-828 inhibits the LPS-induced degradation of the I kappa B alpha and I kappa B beta in THP-1 cells, And CHS-828 uses I kappa B kinase complex as a molecular target of CHS 828. CHS-828 shows cytotoxic effects in OC-NYH small cell lung, PC3 prostatic and in U373MG glioma cell lines, with IC50 values of 0.0003, 0.2, 0.8 nM, respectively.^[1] The inhibition of NF-kappa B transcriptional activity in different cancer cell lines by CHS-828 correlates to some extent with the reduction by CHS -828 of the size of the corresponding xenografts. In vivo, CHS-828 causes a significant regression of NYH tumors in mice: CHS-828 at 20 mg/kg/day caused a reduction in tumor size of 69% (p < 0.0001). And this effect correlates with the inhibition of NF-ΚB activity.^[2] Moreover, CHS-828 has been identified as a Nicotinamide phosphoribosyltransferas (Nampt) inhibitor and inhibits NAD synthesis. And in vitro, CHS-828 inhibits Nampt with an apparent Ki of 2.6 nM.^[3] CHS-828 also inhibits DNA synthesis in NYH small cell lung cancer cells and MCF-7 breast cancer cells. CHS-828 induces an abruptly shut-off DNA synthesis, protein synthesis and cellular proliferation 24??0 hour after exposure, followed by the first signs of cell death.^[4]

Protocols

In vitro, CHS-828 is dissolved in DMSO.^[4]

References

[1] Hjarnaa PJ, et al.CHS 828 a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo.Cancer Res,1999, 59, pp. 5751??757 [2] Olsen, LS, et al. Anticancer agent CHS 828 suppresses nuclear factor??#922;B activity in cancer cells through downregulation of IKK activity. International journal of cancer, 2004, 111(2), 198-205. [3] Olesen UH et al. Anticancer agent CHS-828 inhibits cellular synthesis of NAD Biochem. Biophys. Res. Commun., 2008, 367, pp. 799??04 [4] Ekelund S, et al.Cellular pharmacodynamics of the cytotoxic guanidino-containing drug CHS828. Comparison with methylglyoxal-bis (guanylhdrazone).Eur J Pharmacol, 2001,418, pp. 39??5

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