2. PROTAC Neuronal Signaling
  3. PROTACs α-synuclein
  4. 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.

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Arg-PEG1-Tαsyn

Arg-PEG1-Tαsyn Chemical Structure

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Arg-PEG1-Tαsyn Related Antibodies

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Description

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].

In Vitro

Arg-PEG1-Tα-syn (0-10 μM, 48 h) significantly promotes the reduction of α-synA53T in U251 cells with a DC50 of 0.28 μM, and a Dmax of 90.5% at 5 μM[1].
Arg-PEG1-Tα-syn (1 μM,0-72 h) time-dependently exerts α-synA53T degradation in U251/α-synA53T cells[1].
Arg-PEG1-Tα-syn (1 μM, 48 h) exhibits consistent degradation effects on α-syn in U251/α-synWT, U251/α-synA53T, 293/α-synWT, 293/α-synA53T, SH-SY5Y/α-synWT and SH-SY5Y/α-synA53T cells[1].
Arg-PEG1-Tα-syn induces α-synA53T 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-synWT andα-synA53T 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-synWT or α-synA53T) by reducing α-synA53T aggregation[1].

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

Arg-PEG1-Tαsyn Related Antibodies

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-synWT, U251/α-synA53T, 293/α-synWT, 293/α-synA53T, SH-SY5Y/α-synWT and SH-SY5Y/α-synA53T 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.
Molecular Weight

455.58

Formula

C22H29N7O2S
SMILES

CNC1=CC=C(C2=NC3=CC=C(OCCNC([C@@H](N)CCCNC(N)=N)=O)C=C3S2)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Arg-PEG1-Tαsyn Related Classifications

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Keywords:

Arg-PEG1-TαsynPROTACsα-synucleinα-SynU251 cellsUBR1dopaminergic neuronalParkinson’s diseaseInhibitorinhibitorinhibit

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