Spisulosine
Based on 1 Customer Validation
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation. Spisulosine induces apoptosis in PC-3 and LNCaP cells.
For research use only. We do not sell to patients.
- Purity : 99.5%
- CAS No.: 196497-48-0
- Formula: C18H39NO
- Molecular Weight:285.51
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
[1]|
PKCζ |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HBL-100 | GI50 |
2.3 μM
Compound: 1
|
Antiproliferative activity against human HBL100 cells after 48 hrs incubation by SRB assay
Antiproliferative activity against human HBL100 cells after 48 hrs incubation by SRB assay
|
[PMID: 25899335] |
| HCT-116 | IC50 |
100 nM
Compound: 3; ES-285
|
Cytotoxicity against human HCT-116 cell
Cytotoxicity against human HCT-116 cell
|
[PMID: 31926468] |
| HeLa | GI50 |
2.6 μM
Compound: 1
|
Antiproliferative activity against human HeLa cells after 48 hrs incubation by SRB assay
Antiproliferative activity against human HeLa cells after 48 hrs incubation by SRB assay
|
[PMID: 25899335] |
| HL-60 | IC50 |
100 nM
Compound: 3; ES-285
|
Cytotoxicity against human HL-60 cell
Cytotoxicity against human HL-60 cell
|
[PMID: 31926468] |
| KB | IC50 |
100 nM
Compound: 3; ES-285
|
Cytotoxicity against human KB cell
Cytotoxicity against human KB cell
|
[PMID: 31926468] |
| LNCaP | IC50 |
1 μM
Compound: 3; ES-285
|
Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human LNCaP cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31926468] |
| PC-3 | IC50 |
1 μM
Compound: 3; ES-285
|
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31926468] |
| SW1573 | GI50 |
1.3 μM
Compound: 1
|
Antiproliferative activity against human SW1573 cells after 48 hrs incubation by SRB assay
Antiproliferative activity against human SW1573 cells after 48 hrs incubation by SRB assay
|
[PMID: 25899335] |
| T47D | GI50 |
0.9 μM
Compound: 1
|
Antiproliferative activity against human T47D cells after 48 hrs incubation by SRB assay
Antiproliferative activity against human T47D cells after 48 hrs incubation by SRB assay
|
[PMID: 25899335] |
| WiDr | GI50 |
0.7 μM
Compound: 1
|
Antiproliferative activity against human WiDr cells after 48 hrs incubation by SRB assay
Antiproliferative activity against human WiDr cells after 48 hrs incubation by SRB assay
|
[PMID: 25899335] |
In Vitro
Spisulosine (1 nM-10 μM; 48 h) inhibits the growth of prostate tumor PC-3 and LNCaP cells and human prostate epithelial RWPE-1 cells, and is more effective in PC-3 cells[1].
Spisulosine (1 μM; 48 h) affects the cell cycle, with an increase in the number of sub-G1 cells[1].
Spisulosine (1 μM) induces apoptosis and enhances cleavage of procaspase-3 in PC-3 and LNCaP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC-3, LNCaP and RWPE-1 cells
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Concentration:1 nM, 10 nM, 100 nM, 1 μM 10 μM
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Incubation Time:48 h
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Result:Significantly decreased cell viability.
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Cell Line:PC-3, LNCaP and RWPE-1 cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Showed an increase in the number of sub-G1 cells.
Chemical Information
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CAS No. 196497-48-0
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Appearance Solid
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Molecular Weight 285.51
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Formula C18H39NO
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Color White to off-white
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SMILES
C[C@H](N)[C@H](O)CCCCCCCCCCCCCCC
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Synonyms
ES-285
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 2 mg/mL (7.01 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (267 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5025 mL | 17.5125 mL | 35.0250 mL | 87.5626 mL |
| 5 mM | 0.7005 mL | 3.5025 mL | 7.0050 mL | 17.5125 mL |