DC661

Catalog No.S8808

DC661 Chemical Structure

Molecular Weight(MW): 552.58

DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).

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Biological Activity

Description DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).
Targets
Autophagy [1]
()
In vitro

Treatment of melanoma cells with DC661 results in a more striking accumulation of the autophagic vesicle marker LC3B-II at lower concentrations compared with either Lys05 or HCQ, reflecting more pronounced accumulation of autophagic vesicles at concentrations between 0.1 and 10 μmol/L. All cells die at concentrations above 10 μmol/L for DC661 in contrast to Lys05 and HCQ. Compared with HCQ or Lys05, DC661 treatment induces a significantly more potent inhibition of autophagic flux in melanoma cells expressing the mCherry-eGFP-LC3B reporter, and significantly higher levels of free GFP in melanoma cells expressing GFP-LC3B. DC661 treatment resulted in significantly greater lysosomal deacidification compared with either HCQ or Lys05. The IC50 of DC661 in 72-hour MTT assays is 100-fold lower than that of HCQ across multiple cancer cell lines including colon and pancreas cancer cell lines. DC661 suppresses long-term clonogenic growth of melanoma cells more effectively and induces significantly more apoptosis than Lys05, HCQ, or combined BRAF and MEK inhibition in BRAF-mutant melanoma cells[1].

In vivo

Treatment with the reduced dose (3 mg/kg, i.p.) of DC661 in a HT29 xenograft results in a significant reduction in tumor volume and almost complete suppression of daily tumor growth rate compared with control mice without significantly affecting mouse weight[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: A375P cells
  • Concentrations: 0.1, 0.3, 1, 3, 10 μM
  • Incubation Time: 6 hours
  • Method:

    A375P cells are treated with doses of HCQ, Lys05, or DC661 for 6 hours before lysates are immunoblotted.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: HT29 colorectal xenograft
  • Formulation: water
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL (112.2 mM)
Ethanol 49 mg/mL (88.67 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 552.58
Formula

C31H39Cl2N5

CAS No. 1872387-43-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Can you provide any information on how to formulate this compound for in vivo IP injection?

  • Answer:

    Formula: 5% Stock solution (20 mg/ml)+40% PEG 300+5% Tween80+50% ddH2O, concentration:1mg/ml.

Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID