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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- No. CAS: 3050872-76-6
- Fòrmula: C72H102N10O8S
- Peso molecular:1267.71
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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.
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Cell Line:EOL-1, MV4;11
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Concentration:0.03, 0.1, 0.3 μM
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Incubation Time:24 h
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Result:Did not reduce EZH2 protein levels in EOL-1 cells.
Did not reduce H3K27me3 protein levels in EOL-1 cells.
Chemical Information
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No. CAS 3050872-76-6
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Peso molecular 1267.71
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Fòrmula C72H102N10O8S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS8847N1 Related Classifications
HY-186269 Related Classifications
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