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

PROTAC EED degrader-1 is a von Hippel-Lindau-based 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

CAS No. : 2639882-72-5

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Based on 1 publication(s) in Google Scholar

PROTAC EED degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC EED degrader-1 is a von Hippel-Lindau-based 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[1]

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].

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

PROTAC EED degrader-1 Related Antibodies

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
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (142.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9486 mL 4.7429 mL 9.4859 mL
5 mM 0.1897 mL 0.9486 mL 1.8972 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.75 mg/mL (3.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 3.75 mg/mL (3.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9486 mL 4.7429 mL 9.4859 mL 23.7147 mL
5 mM 0.1897 mL 0.9486 mL 1.8972 mL 4.7429 mL
10 mM 0.0949 mL 0.4743 mL 0.9486 mL 2.3715 mL
15 mM 0.0632 mL 0.3162 mL 0.6324 mL 1.5810 mL
20 mM 0.0474 mL 0.2371 mL 0.4743 mL 1.1857 mL
25 mM 0.0379 mL 0.1897 mL 0.3794 mL 0.9486 mL
30 mM 0.0316 mL 0.1581 mL 0.3162 mL 0.7905 mL
40 mM 0.0237 mL 0.1186 mL 0.2371 mL 0.5929 mL
50 mM 0.0190 mL 0.0949 mL 0.1897 mL 0.4743 mL
60 mM 0.0158 mL 0.0790 mL 0.1581 mL 0.3952 mL
80 mM 0.0119 mL 0.0593 mL 0.1186 mL 0.2964 mL
100 mM 0.0095 mL 0.0474 mL 0.0949 mL 0.2371 mL
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PROTAC EED degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC EED degrader-12639882-72-5PROTAC EED degrader1PROTAC EED degrader 1PROTACsHistone MethyltransferaseInhibitorinhibitorinhibit

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