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MedKoo CAT#: 406969
CAS#: 1391426-24-6
Description: Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications.
MedKoo Cat#: 406969
Name: Lys05 trihydrochloride
CAS#: 1391426-24-6
Chemical Formula: C23H26Cl5N5
Exact Mass: 439.1331
Molecular Weight: 549.75
Elemental Analysis: C, 50.25; H, 4.77; Cl, 32.24; N, 12.74
Related CAS #: 1391426-24-6 (HCl) 1391426-22-4 (free/Lys01)
Synonym: LYS-05 HCl; LYS05; LYS-05; Lys01 (trihydrochloride); Lys01 HCl salt.
IUPAC/Chemical Name: N2-(7-Chloro-4-quinolinyl)-N1-[2-[(7-chloro-4-quinolinyl)amino]ethyl]-N1-methyl-1,2-ethanediamine trihydrochloride
InChi Key: JTUYDBHQGOZPQQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H23Cl2N5.3ClH/c1-30(12-10-28-20-6-8-26-22-14-16(24)2-4-18(20)22)13-11-29-21-7-9-27-23-15-17(25)3-5-19(21)23;;;/h2-9,14-15H,10-13H2,1H3,(H,26,28)(H,27,29);3*1H
SMILES Code: CN(CCNC1=CC=NC2=CC(Cl)=CC=C12)CCNC3=CC=NC4=CC(Cl)=CC=C34.[H]Cl.[H]Cl.[H]Cl
1: Amaravadi RK, Winkler JD. Lys05: a new lysosomal autophagy inhibitor.
Autophagy. 2012 Sep;8(9):1383-4. doi: 10.4161/auto.20958. PubMed PMID: 22878685;
PubMed Central PMCID: PMC3442884.
2: McAfee Q, Zhang Z, Samanta A, Levi SM, Ma XH, Piao S, Lynch JP, Uehara T,
Sepulveda AR, Davis LE, Winkler JD, Amaravadi RK. Autophagy inhibitor Lys05 has
single-agent antitumor activity and reproduces the phenotype of a genetic
autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8. doi:
10.1073/pnas.1118193109. PubMed PMID: 22566612; PubMed Central PMCID: PMC3361415.
3: DeVorkin L, Hattersley M, Kim P, Ries J, Spowart J, Anglesio MS, Levi SM,
Huntsman DG, Amaravadi RK, Winkler JD, Tinker AV, Lum JJ. Autophagy Inhibition
Enhances Sunitinib Efficacy in Clear Cell Ovarian Carcinoma. Mol Cancer Res. 2016
Dec 7. pii: molcanres.0132.2016. [Epub ahead of print] PubMed PMID: 27927774.
4: Shi TT, Yu XX, Yan LJ, Xiao HT. Research progress of hydroxychloroquine and
autophagy inhibitors on cancer. Cancer Chemother Pharmacol. 2016 Nov 26. [Epub
ahead of print] Review. PubMed PMID: 27889812.
