WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407210
Description: EAD1 is a potent and selective autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 had an IC50 of 5.8 μM in the BxPC3 cells and was approximately 8-fold more potent than CQ and HCQ. EAD1 inhibited autophagy, as judged by the cellular accumulation of the autophagy-related autophagosome proteins LC3-II and p62 and induced apoptosis. The increases in LC3-II levels by the analogues were highly correlated with their growth inhibitory IC50s, suggesting that autophagy blockade is closely linked to inhibition of cell proliferation. EAD1 is a viable lead compound for evaluation of the antitumor activity of autophagy inhibitors in vivo.
MedKoo Cat#: 407210
Chemical Formula: C24H27Cl2N7
Exact Mass: 483.1705
Molecular Weight: 484.429
Elemental Analysis: C, 59.51; H, 5.62; Cl, 14.64; N, 20.24
Synonym: EAD1; EAD-1; EAD 1.
IUPAC/Chemical Name: N1-((1-(4-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)-N2-(2-((7-chloroquinolin-4-yl)amino)ethyl)-N2-methylethane-1,2-diamine
InChi Key: NUQMXKCBSUXVTG-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H27Cl2N7/c1-32(13-11-29-23-8-9-28-24-14-20(26)6-7-22(23)24)12-10-27-15-21-17-33(31-30-21)16-18-2-4-19(25)5-3-18/h2-9,14,17,27H,10-13,15-16H2,1H3,(H,28,29)
SMILES Code: ClC1=CC=C2C(N=CC=C2NCCN(C)CCNCC3=CN(CC4=CC=C(Cl)C=C4)N=N3)=C1
1: Nordstrøm LU, Sironi J, Aranda E, Maisonet J, Perez-Soler R, Wu P, Schwartz EL. Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. ACS Med Chem Lett. 2015 Jan 8;6(2):134-9. doi: 10.1021/ml500348p. eCollection 2015 Feb 12. PubMed PMID: 25699157; PubMed Central PMCID: PMC4329578.
2: Kono K, Kuzuya F, Yamamoto T, Endo H. Comparative study of cerebral ventricular dilation and cognitive function in patients with Alzheimer's disease of early versus late onset. J Geriatr Psychiatry Neurol. 1994 Jan-Mar;7(1):39-45. PubMed PMID: 8192829.