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Art. -Nr.: HY-186269

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MS8847N1

MS8847N1 is a negative control analog of MS8847 (HY-162250), which abolishes binding to EZH2 while retaining the activity of recruiting VHL. MS8847N1 does not induce EZH2 degradation. MS8847N1 can be used in PROTAC-related research.
(Pink: EZH2 ligand (HY-186270); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

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CAS. Nr.: 3050872-76-6
Formel: C₇₂H₁₀₂N₁₀O₈S
Molecular Weight:1267.71

Speicherung:

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

MS8847N1 Chemical Structure

CAS. Nr.: 3050872-76-6

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
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Biologische Aktivität

Beschreibung

MS8847N1 is a negative control analog of MS8847 (HY-162250), which abolishes binding to EZH2 while retaining the activity of recruiting VHL. MS8847N1 does not induce EZH2 degradation. MS8847N1 can be used in PROTAC-related research^[1]. (Pink: EZH2 ligand (HY-186270); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

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In Vitro

MS8847N1 is a negative control analog of MS8847 (HY-162250). MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (with a DC₅₀ of 34.4 nM in EOL-1 MLL-rAML cells), which mediates the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models^[1].
MS8847N1 (0.03-0.3 μM; 24 h) does not degrade EZH2 or reduce its H3K27me3 levels in EOL-1 and MV4;11 cells^[1].
MS8847N1 shows no cell growth inhibitory effect after treating MV4;11 cells for 5 days^[1].

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

Western Blot Analysis^[1]

Cell Line:

EOL-1, MV4;11
Concentration:

0.03, 0.1, 0.3 μM
Incubation Time:

24 h
Result:

Did not reduce EZH2 protein levels in EOL-1 cells.
Did not reduce H3K27me3 protein levels in EOL-1 cells.

Chemical Information

CAS. Nr. 3050872-76-6
Molecular Weight 1267.71
Formel C₇₂H₁₀₂N₁₀O₈S
SMILES

CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)CCC(NCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC(C(N(C)CC8=C(C)C=C(C)N(C)C8=O)=O)=C2C
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]. Velez J, et al. Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2. European journal of medicinal chemistry. 2024 Mar 05;267:116154. [Content Brief]

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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100 mg

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Biologische Aktivität
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Chemical Information
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MS8847N1

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