2. PROTAC Stem Cell/Wnt PI3K/Akt/mTOR Neuronal Signaling
  3. PROTACs GSK-3 Tau Protein
  4. PROTAC GSK3 degrader-1

PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease.
(Pink: GSK-3 ligand (HY-185635); Blue: Cereblon ligand (HY-W1137162); Black: linker).

For research use only. We do not sell to patients.

PROTAC GSK3 degrader-1

PROTAC GSK3 degrader-1 Chemical Structure

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PROTAC GSK3 degrader-1 Related Antibodies

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GSK-3 GSK-3α GSK-3β

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Description

PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease[1]. (Pink: GSK-3 ligand (HY-185635); Blue: Cereblon ligand (HY-W1137162); Black: linker).

IC50 & Target[1]

GSK-3β

1.4 nM (DC50)

GSK-3α

 

In Vitro

PROTAC GSK3 degrader-1 (Compound KH1) (10 nM; 2 h) almost completely degrades GSK3α and GSK3β in HEK293 cells, and this degradation depends on the ubiquitin-proteasome system and binding to GSK3[1].
PROTAC GSK3 degrader-1 (0.1-100 nM; 24 h) degrades GSK3β in differentiated SH-SY5Y neuroblastoma cells, with an onset concentration of 0.1 nM; at higher concentrations, it reduces phosphorylated CRMP2 levels and stabilizes β-catenin[1].

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

PROTAC GSK3 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: Differentiated SH-SY5Y neuroblastoma cells
Concentration: 0.1, 1, 10 and 100 nM
Incubation Time: 24 h
Result: Degraded GSK3β at concentrations between 0.1 and 10 nM.
Reduced phospho-CRMP2 levels concurrently with GSK3β degradation.
Stabilized β-catenin most evident at the highest tested concentration of 100 nM.
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration Bioavailability Brain-to-Plasma Ratio
Mice[1] 0.37 mg/kg i.v. > 65 nM 16 nM 1.6 % 0.18
Mice[1] 3.0 mg/kg p.o. / / 1.6 % /
In Vivo

PROTAC GSK3 degrader-1 (Compound KH1) (5 mg/kg; i.v.; single bolus dose) achieves potent, specific degradation of GSK3β in female Balb/c mice, with near-complete removal in liver and significant reduction in brain following a single 5 mg/kg i.v. dose[1].

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

Animal Model: Balb/c (female)[1]
Dosage: 5 mg/kg
Administration: i.v.; single bolus dose
Result: Reduced brain GSK3β levels to ~60% of control levels.
Reduced liver GSK3β levels to ~20% of control levels.
Achieved high proteome-wide specificity for GSK3β removal in liver tissue.
Reduced phosphorylation of GSK3α (Ser21) and AMPK alpha sub-unit (PRKAA1) in liver tissue.
Molecular Weight

898.97

Formula

C47H46N16O4
SMILES

O=C(C1=CC=NN2C1=NC(C3=CC=C(N4N=NC(C5=NC=C(CN6CCN(CC7=CC8=C(C=C7)C(N(C(N9)=O)CCC9=O)=NN8C)CC6)C=C5)=C4)C=C3)=C2)NC%10=C(N%11CCOCC%11)C=CN=C%10
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC GSK3 degrader-1 Related Classifications

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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.

Keywords:

PROTAC GSK3 degrader-1PROTACsGSK-3Tau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3GSK3αβ-cateninubiquitin-proteasome systemHEK293 cellsGSK3βCRMP2TauCereblon E3 ligasePRKAA1SH-SY5Y neuroblastoma cellsInhibitorinhibitorinhibit

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