PI5P4Kγ inhibitor n40

Chemical Structure : PI5P4Kγ inhibitor n40

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货号: PC-27766Not For Human Use, Lab Use Only.

PI5P4Kγ inhibitor n40 is a potent, selective orthosteric-allosteric dual inhibitor of PI5P4Kγ with Kd of 6.55 nM, has >1000-fold selectivity over PI5P4Kα and PI5P4Kβ.

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25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

PI5P4Kγ inhibitor n40 is a potent, selective orthosteric-allosteric dual inhibitor of PI5P4Kγ with Kd of 6.55 nM, has >1000-fold selectivity over PI5P4Kα and PI5P4Kβ.
Compound n40 binds to PI5P4Kγ with ITC Kd of 123 nM.
Compound n40 exhibits potent antiproliferative activity (IC50=0.037 μM, HCC827 cells) and achieves complete inhibition of PI5P4Kγ (100 % inhibition at 500 nM).
Compound n40 is a highly specific inhibitor of PI5P4Kγ in KINOMEscan profiling platform comprising 468 human kinases.
Compound n40 induces apoptosis, effectively suppresses the expression of cell cycle–related proteins on HCC827 cells, also exhibits strong inhibitory effects on EMT and PI3K/AKT/mTOR signaling.
Compound n40 (10, 20 mg/kg) induces dose-dependent tumor growth inhibition of 46.5 % and 62.8 %, respectively, in HCC827 xenograft model.

物理化学性质&存储条件

分子量	364.45
分子式	C21H24N4O2
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	N-(5-(4-oxo-3-propyl-3,4-dihydroquinazolin-6-yl)pyridin-2-yl)pentanamide

参考文献

1. Liang Xiong, et al. J Adv Res. 2026 Jun:84:1105-1126.