1. PROTAC
    Epigenetics
  2. PROTAC
    Histone Methyltransferase
  3. PROTAC EED degrader-2

PROTAC EED degrader-2 

Cat. No.: HY-130615
Handling Instructions

PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.

For research use only. We do not sell to patients.

PROTAC EED degrader-2 Chemical Structure

PROTAC EED degrader-2 Chemical Structure

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Description

PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit[1].

IC50 & Target[1]

VHL

 

In Vitro

PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits PRC2 function with a pIC50 of 8.11±0.09[1].
PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1].
PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].
PROTAC EED degrader-2 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells[1].

Cell Proliferation Assay[1]

Cell Line: Karpas422 cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 4, 8, 12, 14 days
Result: Reduced proliferation. GI50=0.057 μM (Day 14).

Western Blot Analysis[1]

Cell Line: Karpas422 cells
Concentration: 0.1, 1, and 3 μM
Incubation Time: 48 hours
Result: The protein levels of EED, EZH2, H3K27me3 was reduced.

Western Blot Analysis[1]

Cell Line: Karpas422 cells
Concentration: 1 μM
Incubation Time: 1, 2, 4, 6, 8, 24 hours
Result: EED protein levels decreased within 1-2 h of treatment.
Molecular Weight

960.13

Formula

C₅₀H₅₈FN₁₁O₆S

SMILES

FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C4=NN=CN34)C5=C(N=C(C=C5)CCC(NCCCCC(N[[email protected]](C(N6[[email protected]@H](C[[email protected]](C6)O)C(NCC7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)C(C)(C)C)=O)=O)C

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Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PROTAC EED degrader-2PROTAC EED degrader2PROTAC EED degrader 2PROTACHistone MethyltransferaseProteolysis-targeting chimeraProstatebreastcancerPRC2ubiquitindegradationEEDEZH2SUZ12Inhibitorinhibitorinhibit

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PROTAC EED degrader-2
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HY-130615
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