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Cat. No.: 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)).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 3050872-76-6
Formule: C₇₂H₁₀₂N₁₀O₈S
Masse moléculaire:1267.71

Stockage:

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

MS8847N1 Chemical Structure

CAS No.: 3050872-76-6

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Use of MCE Products

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

Activité biologique
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- In Vitro
Chemical Information
Pureté et documentation
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Activité biologique

Description

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)).

Voir tous les produits spécifiques à Isoform PROTACs :

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 No. 3050872-76-6
Masse moléculaire 1267.71
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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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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Activité biologique
- Description
- In Vitro
Chemical Information
Pureté et documentation
Références

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MS8847N1

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