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Art. -Nr.: HY-147174

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PROTAC_ERRα

Name: PROTAC_ERRα
Brand: MedChemExpress
SKU: HY-147174
Price: 450.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC₅₀: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research.
(Pink: ERRα ligand (HY-U00425); Blue: VHL ligand (HY-125845); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.71%
CAS. Nr.: 1801547-15-8
Formel: C₄₆H₄₇F₃N₆O₉S₂
Molecular Weight:949.03

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC_ERRα Chemical Structure

CAS. Nr.: 1801547-15-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC₅₀: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research^[1]^[2]^[3]. (Pink: ERRα ligand (HY-U00425); Blue: VHL ligand (HY-125845); Black: linker).

IC₅₀ & Target^[1]

ERRα

~100 nM (DC₅₀)

VHL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	DC₅₀	100 nM Compound: 12; PROTAC_ERRalpha	Protac activity at VHL/ERRalpha in epoxomicin pre-treated human MCF7 cells assessed as induction of ERRalpha protein degradation incubated for 8 hrs by Western blot analysis Protac activity at VHL/ERRalpha in epoxomicin pre-treated human MCF7 cells assessed as induction of ERRalpha protein degradation incubated for 8 hrs by Western blot analysis	[PMID: 31047748]

In Vitro

PROTAC_ERRα (10-1000 nM; 8 h) potently induces proteasome-dependent degradation of ERRα in breast cancer MCF-7 cells, with a DC₅₀ of approximately 100 nM and a maximum reduction of 86% in protein levels^[1].
PROTAC_ERRα (100-500 nM; 4-24 h) exhibits high specificity for ERRα degradation in MCF-7 breast cancer cells, and only causes additional downregulation of BCR at 500 nM after 24 h of incubation^[1].
PROTAC_ERRα (100 nM) induces a 50% VHL-dependent downregulation of ERRα in MCF7 breast cancer cells^[2].
PROTAC_ERRα induces VHL- and proteasome-dependent, dose-dependent degradation of ERRα in intact cells, with a DC₅₀ of 100 nM^[3].

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

Western Blot Analysis^[1]

Cell Line:

MCF7 cells
Concentration:

0, 10, 30, 100, 300 and 1000 nM
Incubation Time:

8 h
Result:

Decreased in ERRα level in a dose-dependent fashion and the maximal level of degradation (DC₅₀) is 86%.

In Vivo

PROTAC_ERRα (100 mg/kg; i.p.; every eight hours; four total doses) produces significant in vivo knockdown of ERRα in mouse heart, kidney, and MDA-MB-231 xenograft tumors, with reductions ranging from 39% to 44%^[1].

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

Animal Model:

CD-1 (female)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; every eight hours; four total doses
Result:

Reduced ERRα protein levels by 44% in heart tissue compared to vehicle-treated controls.
Reduced ERRα protein levels by 44% in kidney tissue compared to vehicle-treated controls.
Reduced ERRα protein levels by 39% in MDA-MB-231 tumor tissue compared to vehicle-treated controls.

Chemical Information

CAS. Nr. 1801547-15-8
Appearance Solid
Molecular Weight 949.03
Formel C₄₆H₄₇F₃N₆O₉S₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0537 mL

5.2685 mL

10.5371 mL

5 mM

0.2107 mL

1.0537 mL

2.1074 mL

10 mM

0.1054 mL

0.5269 mL

1.0537 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bondeson DP, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nature chemical biology. 2015 Aug;11(8):611-7. [Content Brief]

[2]. Gu S, et al. PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery. Bioessays. 2018 Apr;40(4):e1700247. [Content Brief]

[3]. Coleman K G, et al. Proteolysis-targeting chimeras: harnessing the ubiquitin-proteasome system to induce degradation of specific target proteins[J]. Annual Review of Cancer Biology, 2018, 2: 41-58.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
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Produktname:
CAS. Nr.:
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Reinheit:
Menge:

PROTAC_ERRα

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PROTAC_ERRα Related Classifications

HY-147174 Related Classifications

Bioz