Chemical Structure : GSK3 degrader KH1
CAS No.:
GSK3 degrader KH1
Catalog No.: PC-25840Not For Human Use, Lab Use Only.
GSK3 degrader KH1 is a potent, CNS in vivo active GSK3 PROTAC degrader with DC50 of 1.4 nM in HEK293 cells, induces almost complete GSK3α and GSK3β degradation at 10 nM in HEK293 cells (2 h).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
GSK3 degrader KH1 is a potent, CNS in vivo active GSK3 PROTAC degrader with DC50 of 1.4 nM in HEK293 cells, induces almost complete GSK3α and GSK3β degradation at 10 nM in HEK293 cells (2 h).
GSK3 degrader KH1 mediated GSK3 degradation requires UPS activity and GSK3 engagement.
KH1 demonstrated significant impact on CNS relevant GSK3 substrates in cells.
KH1 (5 mg/kg i.v. dose) was able within 4 h to almost completely remove GSK3β from mouse liver with partial degradation also observed in mouse brain.
Physicochemical Properties
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M.Wt
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898.99
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Formula
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C47H46N16O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(4-(4-(5-((4-((3-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1-methyl-1H-indazol-6-yl)methyl)piperazin-1-yl)methyl)pyridin-2-yl)-1H-1,2,3-triazol-1-yl)phenyl)-N-(4-morpholinopyridin-3-yl)imidazo[1,2-b]pyridazine-8-carboxamide
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References
1. Holmqvist A, et al. Nat Commun. 2025 Oct 6;16(1):8857.
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