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Art. -Nr.: HY-180976

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Arg-PEG1-Tαsyn

Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC₅₀ of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research.
(Pink: α-synuclein ligand (HY-126192); Blue: Arg ligand (HY-N0455); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₂H₂₉N₇O₂S
Molecular Weight:455.58

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Arg-PEG1-Tαsyn Chemical Structure

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC₅₀ of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research^[1]^[2]. (Pink: α-synuclein ligand (HY-126192); Blue: Arg ligand (HY-N0455); Black: linker).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle α-synuclein Isoform-spezifische Produkte anzeigen :

In Vitro

Arg-PEG1-Tα-syn (0-10 μM, 48 h) significantly promotes the reduction of α-syn^A53T in U251 cells with a DC₅₀ of 0.28 μM, and a D_max of 90.5% at 5 μM^[1].
Arg-PEG1-Tα-syn (1 μM,0-72 h) time-dependently exerts α-syn^A53T degradation in U251/α-syn^A53T cells^[1].
Arg-PEG1-Tα-syn (1 μM, 48 h) exhibits consistent degradation effects on α-syn in U251/α-syn^WT, U251/α-syn^A53T, 293/α-syn^WT, 293/α-syn^A53T, SH-SY5Y/α-syn^WT and SH-SY5Y/α-syn^A53T cells^[1].
Arg-PEG1-Tα-syn induces α-syn^A53T reduction, an effect that is reversed by MG132 (HY-13259) but not by Chloroquine (HY-17589A)^[1].
Arg-PEG1-Tα-syn (1 μM, 48 h) mediates the regulation of α-syn^WT andα-syn^A53T via the E3 ubiquitin ligase UBR1 in U251 (knocked down UBR1, UBR2, UBR4, and UBR5 separately using shRNA) cells^[1].
Arg-PEG1-Tα-syn (0-5 μM, 48 h) protects cells from the toxicity induced by α-syn WT or α-syn A53T overexpression in SH-SY5Y cells (overexpressing α-syn^WT or α-syn^A53T) by reducing α-syn^A53T aggregation^[1].

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

Western Blot Analysis^[1]

Cell Line:

U251/α-syn ^A53T cells
Concentration:

1 μM
Incubation Time:

0, 12, 24, 48 and 72 h
Result:

Degraded the α-syn ^A53T as early as 12 h, reaching the peak at 48 h.

Western Blot Analysis^[1]

Cell Line:

U251/α-syn^WT, U251/α-syn^A53T, 293/α-syn^WT, 293/α-syn^A53T, SH-SY5Y/α-syn^WT and SH-SY5Y/α-syn^A53T cells
Concentration:

1 μM
Incubation Time:

48 h
Result:

Triggered efficient reduction of α-syn ^WT or α-syn ^A53T.

Western Blot Analysis^[1]

Cell Line:

U251 cells (knocked down UBR1, UBR2, UBR4, and UBR5 separately using shRNA)
Concentration:

1 μM
Incubation Time:

48 h
Result:

Induced the degradation of both α-syn ^A53T and α-syn ^WT in U251 cells, an effect that is markedly suppressed by UBR1 knockdown but barely affected by UBR2, UBR4, or UBR5 knockdown.

Cell Viability Assay^[1]

Cell Line:

SH-SY5Y cells (overexpressing α-syn ^WT or α-syn ^A53T)
Concentration:

0, 1 and 5 μM
Incubation Time:

48 h
Result:

Significantly enhanced cell viability in α-syn WT cells at 5 μM and in α-syn A53T cells starting at 1 μM.

Immunofluorescence^[1]

Cell Line:

SH-SY5Y cells
Concentration:

5 μM
Incubation Time:

48 h
Result:

Significantly reduced α-syn A53T aggregates.
Reduced α-syn A53T aggregates.

In Vivo

Arg-PEG1-Tα-syn (mixed with OP50 bacteria at varying concentrations for feeding, p.o., from the L1 larval stage to day-5 adulthood) decreases α-syn aggregates, significantly improves the morphology of neuronal cell bodies and synapses and partially restore the dopaminergic neuronal functional deficits induced by α-syn pathology in C. elegans NL5901^[1].
Arg-PEG1-Tα-syn (0-10 μM were mixed with OP50 bacteria for feeding, p.o., from the L1 larval stage to day-5 adulthood) effectively ameliorates locomotor dysfunction induced by α-syn pathology in a dose-dependent manner in C. elegans overexpressing human α-syn A53T. with safety profile (5 μM) in C. elegans UM0020 and C. elegans (W.T.) ^[1].

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

Animal Model:

C. elegans UM0020 (A537 mutant) and C. elegans NL5901 (W.T.)^[1]
Dosage:

0, 5 and 10 μM
Administration:

p.o., om the L1 larval stage to day-5 adulthood
Result:

Significantly rescued the locomotor deficits of UM0020 worms at day-1 and day-5 of adulthood, with a more pronounced effect at day-5.
Significantly improved the locomotor performance of UM0020 worms at 1 μM.

Animal Model:

C. elegans UM0020 and C. elegans NL5901 (W.T.)^[1]
Dosage:

5 μM
Administration:

p.o., om the L1 larval stage to day-5 adulthood
Result:

Has no significant difference in thrashing frequency.

Chemical Information

Molecular Weight 455.58
Formel C₂₂H₂₉N₇O₂S
SMILES

CNC1=CC=C(C2=NC3=CC=C(OCCNC([C@@H](N)CCCNC(N)=N)=O)C=C3S2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Shen L, et al. Targeted degradation of α-synuclein by arginine-based PROTACs. J Biol Chem. 2025 Aug;301(8):110449. [Content Brief]

[2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]

Calculators

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)}

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.

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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Arg-PEG1-Tαsyn

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle α-synuclein Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Arg-PEG1-Tαsyn Related Classifications

HY-180976 Related Classifications