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Art. -Nr.: HY-187705

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SE486-11

SE486-11 is an orally active USP5 inhibitor. SE486-11 increases free polyubiquitin chains and promotes the ubiquitination and degradation of MYCN. The combination of SE486-11 with SAHA (HY-10221) synergistically induces Apoptosis. SE486-11 can be used in research related to MYCN-driven neuroblastoma.

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CAS. Nr.: 305333-99-7
Formel: C₂₆H₂₀N₄O
Molecular Weight:404.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

SE486-11 Chemical Structure

CAS. Nr.: 305333-99-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Kelly	IC50	34.4 μM	Cytotoxicity against human neuroblastoma Kelly cells by Alamar Blue cell viability assay. Cytotoxicity against human neuroblastoma Kelly cells by Alamar Blue cell viability assay.	37060785

In Vitro

SE486-11 (1:5 ratio with SAHA) binds purified full-length USP5 protein with a K_d of 159 nM, over 100-fold higher affinity than SAHA alone^[1].
SE486-11 does not exhibit measurable binding affinity to purified full-length USP5 protein in an MST assay, as a dose-response kinetic curve could not be fitted^[2].
SE486-11 (5-10 µM; 48-72 h) causes synergistic cytotoxicity in MYCN-amplified neuroblastoma cells (SK-N-BE(2)-C, Kelly, CHP134, IMR-32, LAN-1) and MDA-MB-231 breast cancer cells, with limited effects on normal human fibroblasts (WI-38, MRC-5)^[1].
SE486-11 (5 µM; 24-72 h) reduces clonogenic colony formation (number and size) in MYCN-amplified SK-N-BE(2)-C and Kelly neuroblastoma cells^[1].
SE486-11 inhibits the viability of SK-N-BE(2)-C and Kelly human neuroblastoma cells with IC₅₀ values of 41.8 μM and 34.4 μM, respectively^[2].
SE486-11 enhances the effectiveness of HDAC inhibitors in neuroblastoma cells by increasing MYCN ubiquitination via modulation of USP5^[2].
SE486-11 (5 µM; 72 h) synergistically induces apoptosis in MYCN-amplified SK-N-BE(2)-C and Kelly neuroblastoma cells, but not in normal WI-38 and MRC-5 human fibroblasts^[1].
SE486-11 (5 µM; 48 h) increases mitochondrial depolarisation in MYCN-amplified SK-N-BE(2)-C and Kelly neuroblastoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MDA-MB-231 breast cancer cells, SK-N-BE(2)-C and Kelly MYCN-amplified neuroblastoma cells, WI-38 and MRC-5 normal human fibroblasts, panel of MYCN-amplified (CHP134, IMR-32, LAN-1) and non-amplified (SH-SY5Y, SK-N-AS, SK-N-FI) neuroblastoma cells
Concentration:

10 µM (with 1.9 µM SAHA, MDA-MB-231 cells); 5 µM (with 1 µM SAHA, SK-N-BE(2)-C, Kelly, WI-38, MRC-5 cells and neuroblastoma cell panel)
Incubation Time:

48 h (MDA-MB-231 cells and neuroblastoma cell panel); 72 h (SK-N-BE(2)-C, Kelly, WI-38, MRC-5 cells)
Result:

Reduced MDA-MB-231 cell viability to <40% when used with 1.9 µM SAHA for 48 h, while maintaining >70% viability when used alone.
Caused synergistic cytotoxicity (combination index <1) and reduced cell viability far below single agents in MYCN-amplified neuroblastoma cells when used with 1 µM SAHA for 72 h.
Exhibited limited cytotoxicity in normal WI-38 and MRC-5 fibroblasts when used with 1 µM SAHA for 72 h.
Caused the greatest viability reduction in MYCN-amplified neuroblastoma lines compared to non-amplified lines when used with 1 µM SAHA for 48 h.

Apoptosis Analysis^[1]

Cell Line:

SK-N-BE(2)-C and Kelly MYCN-amplified neuroblastoma cells, WI-38 and MRC-5 normal human fibroblasts
Concentration:

5 µM (with 1 µM SAHA)
Incubation Time:

72 h
Result:

Significantly increased the percentage of cells in early and late apoptosis in SK-N-BE(2)-C and Kelly cells compared to single agents or DMSO control.
Did not induce apoptosis in normal WI-38 and MRC-5 fibroblasts.

In Vivo

Combination treatment with SE486-11 (30 mg/kg; i.p.; 5 days on/2 days off; 21 days) and Suberoylanilide hydroxamic acid (HY-10221) completely blocks tumour formation in homozygous TH-MYCN^+/+ neuroblastoma transgenic mice^[1].
Combination treatment with SE486-11 (30 mg/kg; p.o.; daily; 7 days) and SAHA reduces tumour size and lowers MYCN, USP5, and proliferation marker PCNA levels in MYCN-transgenic zebrafish with neuroblastoma^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

TH-MYCN+/+ (female, 3 weeks old, transgenic spontaneously developing neuroblastoma)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; 5 days on/2 days off; 21 days
Result:

Reduced tumour formation to the extent that no tumour tissue remained for histopathological analysis.

Animal Model:

dβh:EGFP-MYCN (0.5-1.5 years old, transgenic GFP-positive neuroblastoma)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; daily; 7 days
Result:

Caused a reduction in GFP-positive tumour size from day 1 to day 7.
Reduced MYCN, USP5, and PCNA protein levels in tumour tissue compared with vehicle control.

Chemical Information

CAS. Nr. 305333-99-7
Molecular Weight 404.46
Formel C₂₆H₂₀N₄O
SMILES

CC1=C(C#N)C2=NC3=C(C=CC=C3)N2C(NC4=CC=C(O)C=C4)=C1CC5=CC=CC=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Cheung BB, et al. A novel combination therapy targeting ubiquitin-specific protease 5 in MYCN-driven neuroblastoma. Oncogene. 2021 Apr;40(13):2367-2381.

[2]. Gadde S, et al. Pyrimido[1,2-a]benzimidazoles as inhibitors of oncoproteins ubiquitin specific protease 5 and MYCN in the childhood cancer neuroblastoma. Bioorg Chem. 2023 Jul;136:106462.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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SE486-11

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