GSK3 degrader KH1

Chemical Structure : GSK3 degrader KH1

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货号: 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).

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	898.99
分子式	C47H46N16O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Holmqvist A, et al. Nat Commun. 2025 Oct 6;16(1):8857.