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  3. PBA-1105 TFA

PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 TFA selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 TFA increases the autophagic flux of Ub-conjugated aggregates.

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PBA-1105 TFA Chemical Structure

PBA-1105 TFA Chemical Structure

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Description

PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 TFA selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 TFA increases the autophagic flux of Ub-conjugated aggregates[1].

In Vitro

PBA-1105 TFA induces autophagic degradation of stably expressed mutant tau at DC50 of 0.71 nM and Dmax,24 hr of 100 nM, followed by a hook effect at higher concentrations[1].
PBA-1105 (0.1-10 μM; 24 hours) TFA induces the autophagic degradation of misfolded proteins and aggregates at nanomolar concentrations. PBA-1105 TFA leads to significant degradation of mutant tau and misfolded proteins[1].

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

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Activated p62 oligomerization and increased autophagic flux of ubiquitinated aggregates.

Western Blot Analysis[1]

Cell Line: SH-SY5Y-tauP301L cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: Selectively degraded mutant tauP301L with a DC50 of 0.71 nM and persistently cleared insoluble tau aggregates.
In Vivo

PBA-1105 (20-50 mg/kg; intraperitoneal injection; three times per week; for 4 weeks) TFA successfully reduces tau aggregation and oligomeric species in a transgenic mouse model of tauopathies[1].

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

Animal Model: hTauP301L-BiFC transgenic mice[1]
Dosage: 20 mg/kg or 50 mg/kg (PBS containing 30% polyethylene glycol (PEG))
Administration: Intraperitoneal injection; three times per week; for 4 weeks
Result: Effectively cleared tau aggregates in a dose-dependent manner, significantly reducing insoluble tau species in the brain while leaving soluble tau species unaffected.
Resulted in increased levels of autophagic markers like LC3, confirming the activation of autophagic degradation pathways.
Immunohistochemical analysis showed a marked reduction in tau oligomers and phosphorylated tau in both cortical and hippocampal regions.
Molecular Weight

754.83

Formula

C41H49F3N2O8

Appearance

Oil

SMILES

O=C(O)C(F)(F)F.O=C(CCCC1=CC=CC=C1)NCCOCCOCCOCCNCC2=CC(OCC3=CC=CC=C3)=C(OCC4=CC=CC=C4)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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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.

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Product Name:
PBA-1105 TFA
Cat. No.:
HY-161743A
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