Chemical Structure : PI5P4Kγ inhibitor n40
CAS No.:
3112107-90-8
PI5P4Kγ inhibitor n40
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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364.45
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Formula
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C21H24N4O2
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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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N-(5-(4-oxo-3-propyl-3,4-dihydroquinazolin-6-yl)pyridin-2-yl)pentanamide
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References
1. Liang Xiong, et al. J Adv Res. 2026 Jun:84:1105-1126.
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