PROTAC ERRα Degrader-3

Name: PROTAC ERRα Degrader-3
Brand: MedChemExpress
SKU: HY-139185
Rating: 4.5 (1 reviews)

Cat. No.: HY-139185 Purity: 98.49%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.

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

PROTAC ERRα Degrader-3 Chemical Structure

CAS No. : 2306388-65-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 330	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 330	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 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 Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ERRα

VHL

In Vitro

PROTAC ERRα Degrader-3 (compound 6c; 0.3 nM-10 μM; 4 hours) dose-dependently induces ERRα degradation with an efficacious dose as low as 3.0 nM at 4.0 h. PROTAC ERRα Degrader-3 potently decreases protein levels of ERRα downstream target genes, e.g., ATP5B, medium-chain acyl CoA dehydrogenase (MCAD), and pyruvate dehydrogenase kinase 4 (PDK4) in the MDA-MB-231 cells after a 24 h treatment^[1].
PROTAC ERRα Degrader-3 exhibits an IC₅₀ value of 12.67 nM to block the protein-protein interaction of ERRα with PGC-1α peptide and induces approximately 96% protein degradation at 100 nM (D100 nM) after 4.0 h treatment^[1].

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

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
Incubation Time:	4 hours
Result:	Dose-dependently induced ERRα degradation.

Molecular Weight

956.99

Formula

C₄₇H₅₀F₆N₆O₇S

CAS No.

2306388-65-6

Appearance

Solid

Color

Off-white to light yellow

SMILES

COC(C=C1/C=C(C#N)/C(NCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)=O)=O)=O)=C(C=C1)OCC5=C(C=C(C=C5)C(F)(F)F)C(F)(F)F

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 : 80 mg/mL (83.60 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	1.0449 mL	5.2247 mL	10.4494 mL
5 mM	0.2090 mL	1.0449 mL	2.0899 mL
10 mM	0.1045 mL	0.5225 mL	1.0449 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.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (2.09 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 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.

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).

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: 98.82%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (249 KB) HNMR (269 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Lijie Peng, et al. Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation. ACS Med Chem Lett. 2019 Apr 12;10(5):767-772. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0449 mL	5.2247 mL	10.4494 mL	26.1236 mL
	5 mM	0.2090 mL	1.0449 mL	2.0899 mL	5.2247 mL
	10 mM	0.1045 mL	0.5225 mL	1.0449 mL	2.6124 mL
	15 mM	0.0697 mL	0.3483 mL	0.6966 mL	1.7416 mL
	20 mM	0.0522 mL	0.2612 mL	0.5225 mL	1.3062 mL
	25 mM	0.0418 mL	0.2090 mL	0.4180 mL	1.0449 mL
	30 mM	0.0348 mL	0.1742 mL	0.3483 mL	0.8708 mL
	40 mM	0.0261 mL	0.1306 mL	0.2612 mL	0.6531 mL
	50 mM	0.0209 mL	0.1045 mL	0.2090 mL	0.5225 mL
	60 mM	0.0174 mL	0.0871 mL	0.1742 mL	0.4354 mL
	80 mM	0.0131 mL	0.0653 mL	0.1306 mL	0.3265 mL