DiOC5(3) (solution)
DiOC5(3) (solution) is a mitochondrial Fluorescent dye that alters membrane potential, and it also acts as an inhibitor of NADH-ubiquinone reductase (respiratory complex I). DiOC5(3) (solution) increases the NADH/NAD ratio and induces excessive production of ROS. DiOC5(3) (solution) induces Apoptosis. DiOC5(3) accumulates in the mitochondria of leukemia stem-like cells via organic anion-transporting polypeptides, specifically labels these cells, and inhibits their proliferation. DiOC5(3) (solution) enhances the cellular uptake of Hoechst 33342 (HY-15559), reduces Hoechst 33342-associated cytotoxicity, and improves the resolution of DNA content analysis by flow cytometry. DiOC5(3) (solution) shows no detectable fluorescence signal when excited in the 400-500 nm ultraviolet light range. DiOC5(3) (solution) is applicable to leukemia-related research.
For research use only. We do not sell to patients.
- CAS No.: 53213-81-3
- Formula: C27H33IN2O2
- Molecular Weight:544.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
0.29 μM
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Inhibition of cell proliferation against human chronic myelogenic leukemia K562 ALDH+ cells assessed via luminescent viability assay.
Inhibition of cell proliferation against human chronic myelogenic leukemia K562 ALDH+ cells assessed via luminescent viability assay.
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25818410 |
| K562 | IC50 |
0.68 μM
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Inhibition of cell proliferation against human chronic myelogenic leukemia K562 ALDH- cells assessed via luminescent viability assay.
Inhibition of cell proliferation against human chronic myelogenic leukemia K562 ALDH- cells assessed via luminescent viability assay.
|
25818410 |
In Vitro
DiOC5(3) (solution) (300 nM; 48 h) selectively stains and inhibits the proliferation of K562 ALDH+ leukemia stem-like cells with an IC50 of 0.29 μM. It exhibits lower potency against K562 ALDH- cells (IC50 0.68 μM) and exerts minimal toxicity to normal HUCB CD34+ progenitor cells, cells derived from zebrafish embryos, adult zebrafish blood cells, and developing zebrafish embryos[1].
DiOC5(3) (solution) (200 nM; 24 h) increases the NADH/NAD+ ratio in the mitochondria of K562 cells, elevates intracellular ROS levels, preferentially induces apoptosis in K562 ALDH+ leukemic stem-like cells, and simultaneously regulates the expression of CML-related genes, stem cell-associated genes, and anticancer genes[1].
DiOC5(3) (solution) (200 nM; 24 h) preferentially alters the expression of genes associated with key cellular processes in K562 ALDH+ leukemia stem-like cells, and exerts a subpopulation-specific effect on the NF-κB pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human chronic myelogenic leukemia K562 ALDH+, K562 ALDH-, human umbilical cord blood (HUCB) CD34+ progenitor cells, zebrafish embryo-derived cells, adult zebrafish blood cells (ZBCs)
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Concentration:300 nM
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Incubation Time:48 h (300 nM treatment; zebrafish embryo treatment)
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Result:Accumulated in K562 ALDH+ cells at a significantly higher rate than in K562 ALDH- and HUCB CD34+ cells (P < 0.01).
Suppressed K562 ALDH+ cell proliferation to a significantly greater degree than K562 ALDH- and HUCB CD34+ cells (P < 0.01), with a lower IC50 for ALDH+ cells than ALDH- cells (P < 0.05).
Exhibited higher cytotoxicity thresholds for non-cancer cells (ZBCs and HUCB CD34+ cells) compared to K562 cells.
Caused no death or phenotypic changes in zebrafish embryos treated from 48 hpf for 48 h, except for whole-body green-fluorescent staining.
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Cell Line:K562 ALDH+, K562 ALDH-, isolated K562 cell mitochondria
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Concentration:200 nM
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Incubation Time:24 h
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Result:Significantly increased the NADH/NAD+ ratio in isolated K562 mitochondria (P < 0.05), indicating inhibition of NADH-ubiquinone reductase activity.
Increased ROS levels in both K562 ALDH+ and ALDH- subpopulations (P < 0.01), with a higher increase ratio in ALDH+ cells.
Increased apoptotic cells in both subpopulations (P < 0.01), with ALDH+ cells showing greater sensitivity (P < 0.01 vs.
ALDH- cells).
Downregulated expression of BCR-ABL, SIRT1, CD44, and CD133 (P < 0.01 or P < 0.05) and upregulated expression of TP53 and CDKN1A (P < 0.01) in both ALDH+ and ALDH- cells.
In Vivo
Exposure of normally developing zebrafish embryos to DiOC5(3) (solution) (1 μM) for 48 h does not show any developmental toxicity or lethality[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nacre/rose/fli1:egfp (48-hpf, xenotransplanted with human chronic myelogenic leukemia K562 ALDH+ putative leukemia stem-like cells into yolk sac)[1]
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Dosage:0.5 μM (proliferation inhibition); 10 μM (selective staining and proliferation inhibition)
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Administration:continuous exposure in E3 medium; 48 hours (0.5 μM); yolk sac injection; single dose (10 μM)
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Result:Significantly inhibited proliferation of ALDH+ leukemia stem-like cells (P < 0.01 vs. control) with selective activity relative to ALDH- leukemia cells (P < 0.05).
Selectively stained ALDH+ cells 1 hour post-injection (DiOC5(3)/KOr fluorescence ratio was significantly higher in ALDH+ vs.
ALDH- xenografts, P < 0.01).
Caused a greater reduction in ALDH+ cell proliferation over 48 hours (P < 0.05 vs.
ALDH- cells).
Induced significant decreases in ALDH+ cell fluorescence observed at 12, 24, 36, and 48 hours post-injection (P < 0.05 or P < 0.01 vs. 1 hour post-injection).
Chemical Information
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CAS No. 53213-81-3
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Molecular Weight 544.47
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Formula C27H33IN2O2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Zhang B, et al. In vivo selective imaging and inhibition of leukemia stem-like cells using the fluorescent carbocyanine derivative, DiOC5(3). Biomaterials. 2015 Jun;52:14-25. [Content Brief]
[2]. Crissman HA, et al. Supravital cell staining with Hoechst 33342 and DiOC5(3). Methods Cell Biol. 1990;33:89-95. . [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DiOC5(3) (solution) Related Classifications
HY-DY1114 Related Classifications
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Keywords
- DiOC5(3) (solution)
- 53213-81-3
- Fluorescent Dye
- Reactive Oxygen Species (ROS)
- Mitochondrial Metabolism
- Apoptosis
- leukemia stem-like cells
- K562 ALDH+ leukemia stem-like cells
- SLCO4C1
- SLCO4A1
- respiratory complex I
- NADH-ubiquinone reductase
- NF-κB
- human umbilical cord blood CD34 progenitor cells
- zebrafish
- reactive oxygen species
- Inhibitor
- inhibitor
- inhibit