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

PROTAC EED degrader-1 

Cat. No.: HY-130614
Handling Instructions

PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.

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

PROTAC EED degrader-1 Chemical Structure

PROTAC EED degrader-1 Chemical Structure

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Description

PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].

IC50 & Target

VHL

 

In Vitro

PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits PRC2 function with a pIC50 of 8.17±0.24[1].
PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1].
PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].
PROTAC EED degrader-1 (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, 100μM
Incubation Time: 4, 8, 12, 14 days
Result: Reduced proliferation. GI50=0.045 uM (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

1054.20

Formula

C₅₅H₆₀FN₁₁O₈S

SMILES

FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C4=C(C)N=C(CCC(NCCOC5=CC=C(OCC(N[[email protected]@H](C(C)(C)C)C(N6[[email protected]](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[[email protected]@H](O)C6)=O)=O)C=C5)=O)C=C4)C9=NN=CN39

Shipping

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-1PROTAC EED degrader1PROTAC EED degrader 1PROTACHistone MethyltransferaseProteolysis-targeting chimeraProstatebreastcancerPRC2ubiquitindegradationEEDEZH2SUZ12Inhibitorinhibitorinhibit

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PROTAC EED degrader-1
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HY-130614
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