EAD1
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.
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.
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.
| Chemical | |
|---|---|
| CAS Num | 1644388-26-0 |
| Chemical Formula | C24H27Cl2N7 |
| Molecular Weight | 484.429 |
| 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 |
| Exact Mass | 483.1705 |
| Elemental Analysis | C, 59.51; H, 5.62; Cl, 14.64; N, 20.24 |
| Synonym | EAD1; EAD-1; EAD 1. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | ClC1=CC=C2C(N=CC=C2NCCN(C)CCNCC3=CN(CC4=CC=C(Cl)C=C4)N=N3)=C1 |
| Biological | |
| Targets and Effects | Autophagy inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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