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PROTAC ERRα Degrader-3 

Cat. No.: HY-139185 Purity: 98.82%
Handling Instructions

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

PROTAC ERRα Degrader-3 Chemical Structure

CAS No. : 2306388-65-6

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5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
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25 mg USD 950 In-stock
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50 mg USD 1450 In-stock
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100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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].

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.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References

Purity: 98.82%

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Product Name:
PROTAC ERRα Degrader-3
Cat. No.:
HY-139185
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