PROTAC EED degrader-2

Name: PROTAC EED degrader-2
Brand: MedChemExpress
SKU: HY-130615
Rating: 4.5 (1 reviews)

Cat. No.: HY-130615 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pK_D 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

CAS No. : 2639882-69-0

Size	Price	Stock	Quantity
1 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
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
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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

IC₅₀ & Target^[1]

VHL

Cellular Effect

Cell Line	Type	Value	Description	References
KARPAS-422	GI₅₀	57 nM Compound: 106; PROTAC 1	Antiproliferative activity against human Karpas422 cells after 14 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Karpas422 cells after 14 days by celltiter-glo luminescent cell viability assay	[PMID: 33283516]
KARPAS-422	GI₅₀	57 nM Compound: 72	Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition measured after 7 to 10 days by celltitre-glo-luminescent assay Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition measured after 7 to 10 days by celltitre-glo-luminescent assay	[PMID: 35093670]

In Vitro

PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pK_D 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].

MedChemExpress (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.

2639882-69-0

Appearance

Solid

Color

White to off-white

SMILES

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

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 : 80 mg/mL (83.32 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	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

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (2.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (2.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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).

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

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

Purity: 99.90%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Hsu JH, et al. EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex. Cell Chem Biol. 2019 Nov 26. pii: S2451-9456(19)30362-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0415 mL	5.2076 mL	10.4153 mL	26.0381 mL
	5 mM	0.2083 mL	1.0415 mL	2.0831 mL	5.2076 mL
	10 mM	0.1042 mL	0.5208 mL	1.0415 mL	2.6038 mL
	15 mM	0.0694 mL	0.3472 mL	0.6944 mL	1.7359 mL
	20 mM	0.0521 mL	0.2604 mL	0.5208 mL	1.3019 mL
	25 mM	0.0417 mL	0.2083 mL	0.4166 mL	1.0415 mL
	30 mM	0.0347 mL	0.1736 mL	0.3472 mL	0.8679 mL
	40 mM	0.0260 mL	0.1302 mL	0.2604 mL	0.6510 mL
	50 mM	0.0208 mL	0.1042 mL	0.2083 mL	0.5208 mL
	60 mM	0.0174 mL	0.0868 mL	0.1736 mL	0.4340 mL
	80 mM	0.0130 mL	0.0651 mL	0.1302 mL	0.3255 mL