Synonym: Lys-01 3HCl; Lys-05; Lys01 3HCl; N-(7-Chloroquinolin-4-yl)-N′-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N′-methylethane-1,2-diamine trihydrochloride; N1-(7-Chloroquinolin-4-yl)-N2-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N2-methylethane-1,2-diamine trihydrochloride; PS-1001; PS1001
CAS Number: 1391426-24-6
Empirical Formula (Hill Notation): C23H23Cl2N5 · 3HCl
Molecular Weight: 549.75
Linear Formula: C23H23Cl2N5 · 3HCl
Product Type: Chemical
| assay |
≥98% (HPLC) |
| color |
white to beige |
| form |
powder |
| InChI key |
JTUYDBHQGOZPQQ-UHFFFAOYSA-N |
| SMILES string |
[Cl-].[Cl-].[Cl-].Clc1cc2nccc(c2cc1)[N+H2]CC[N+H](CC[N+H2]c3c4c(ncc3)cc(cc4)Cl)C |
| solubility |
DMSO: 2 mg/mL, clear |
| storage condition |
desiccated |
| storage temp. |
−20°C |
| Application: |
Lys05 has been used as an autophagy inhibitor to study its interactions with piperazine. It has also been used as a lysosomal inhibitor to study its effects on myogenesis in Gallus gallus. |
| Biochem/physiol Actions: |
Dimeric chloroquine (CQ) with higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ both in vitro and in vivo. |
| Biochem/physiol Actions: |
Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15.4 post 4 hr 10 μM treatment in LN229 glioblastoma cells vs. <6.4 with 100 μM CQ or HCQ). Lys05 also shows higher anticancer activity both in vitro (IC50 3.6-6.0 μM vs. 15.6-23.8 μM with HCQ in 1205Lu, c8161, LN229, HT-29 cultures) and in mice in vivo (EC50 in reducing tumor growth rate ∼10 mg/kg/day i.p.; HT29 xenografts) with toxicity observed only at high doses (≥80 mg/kg) as a result of significant lysozyme reduction. |
| RIDADR |
NONH for all modes of transport |
| WGK Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
≥98% (HPLC) |
| Storage Temp. |
−20°C |
| UNSPSC |
12352200 |
