2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. PROTAC_ERRα

PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker.

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PROTAC_ERRα Chemical Structure

PROTAC_ERRα Chemical Structure

CAS No. : 1801547-15-8

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Based on 1 publication(s) in Google Scholar

PROTAC_ERRα Related Antibodies

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Description

PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker[1].

In Vitro

PROTAC_ERRα (0-1000 nM; 8 hours; MCF7 cells) down-regulates ERRα protein levels in a dose-dependent fashion[1].
PROTAC_ERRα (100-500 nM; 4-24 hours; MCF7 cells) possesses good selectivity for ERRα target and decreases protein levels of ERRα downstream target genes[1].

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

PROTAC_ERRα Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 0, 10, 30, 100, 300 and 1000 nM
Incubation Time: 8 hours
Result: Decreased in ERRα level in a dose-dependent fashion and the maximal level of degradation (D50) is 86%.
In Vivo

PROTAC_ERRα (100 mg/kg; i.p.; every eight hours) degrades ERRα level in vivo[1].

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

Animal Model: Female CD-1 mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection ; every eight hours.
Result: Reduced ERRα levels in mouse heart and kidney and MDA-MB-231 tumors by approximately 44%, 44% and 39%, respectively.
Molecular Weight

949.03

Formula

C46H47F3N6O9S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(/C(SC1=O)=C/C2=CC(OC)=C(C=C2)OC3=C(C=C(C=C3)C#N)C(F)(F)F)N1CCOCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (131.71 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 1.0537 mL 5.2685 mL 10.5371 mL
5 mM 0.2107 mL 1.0537 mL 2.1074 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
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 1.0537 mL 5.2685 mL 10.5371 mL 26.3427 mL
5 mM 0.2107 mL 1.0537 mL 2.1074 mL 5.2685 mL
10 mM 0.1054 mL 0.5269 mL 1.0537 mL 2.6343 mL
15 mM 0.0702 mL 0.3512 mL 0.7025 mL 1.7562 mL
20 mM 0.0527 mL 0.2634 mL 0.5269 mL 1.3171 mL
25 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
30 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8781 mL
40 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6586 mL
50 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5269 mL
60 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL
80 mM 0.0132 mL 0.0659 mL 0.1317 mL 0.3293 mL
100 mM 0.0105 mL 0.0527 mL 0.1054 mL 0.2634 mL
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PROTAC_ERRα 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_ERRα1801547-15-8PROTACsEpigenetic Reader DomainERRαproteasomaldegraderInhibitorinhibitorinhibit

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