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

PROTAC EED degrader-2 

Cat. No.: HY-130615 Purity: 98.64%
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

CAS No. : 2639882-69-0

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5 mg USD 950 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 3450 In-stock
Estimated Time of Arrival: December 31
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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].

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

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

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (104.15 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0415 mL 5.2076 mL 10.4153 mL
5 mM 0.2083 mL 1.0415 mL 2.0831 mL
10 mM 0.1042 mL 0.5208 mL 1.0415 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 10 mg/mL (10.42 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 10 mg/mL (10.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
PROTAC EED degrader-2
Cat. No.:
HY-130615
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