Lys05

SKU: orb1226383

Description

Lys05 (Lys01 trihydrochloride, PS-1001) is the water-soluble salt of Lys01, is a 10-fold more potent lysosomal autophagy inhibitor than hydroxychloroquine (HCQ); shows IC50 values of 3.6, 3.8, 6 and 7.9 uM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay; more potently accumulates within and deacidifies the lysosome, resulting in impaired autophagy and tumor growth; enhances sunitinib-mediated suppression of clear cell ovarian carcinoma (CCOC) cell viability.

Key Properties

• CAS Number: 1391426-24-6
• MW: 549.75
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₆Cl₅N₅
• SMILES: CN(CCNC1=CC=NC2=CC(Cl)=CC=C12)CCNC3=CC=NC4=CC(Cl)=CC=C34.[H]Cl.[H]Cl.[H]Cl
• Target: Autophagy
• Solubility: DMSO: 6.4 mg/mL, Need Ultrasonic; Water: 3 mg/mL (5.5 mM); Ethanol: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with Lys05 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in Lys05-treated tumors. Tumor growth is significantly impaired in Lys05-treated tumors compared with controls. Lys05 treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three-and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ-and Lys05-treated tumors, respectively, compared with control-treated tumors.
• In Vitro:
  Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and Lys05 produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lys-05 | Lys 05 | Lys01 trihydrochloride | PS-1001

Quick Database Links

Gene Symbol

Autophagy