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VPS34 inhibitor 1 (Compound 19, PIK-III analogue)

Catalog No. T7944 CAS 1383716-46-8

Synonyms: PIK-III analogue

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)

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VPS34 inhibitor 1 (Compound 19, PIK-III analogue) Chemical Structure

VPS34 inhibitor 1 (Compound 19, PIK-III analogue), CAS 1383716-46-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
2 mg	In stock	$ 123.00
5 mg	In stock	$ 223.00
10 mg	In stock	$ 343.00
25 mg	In stock	$ 579.00
50 mg	In stock	$ 829.00
100 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 223.00

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Purity: 98.44%

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Description	VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)
Targets&IC50	VPS34:15 nM
In vitro	VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is extraordinarily selective over other lipid and protein kinases. The ability of compound 19 to prevent the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1 is similar to PIK-III. In addition, treatment of cells with compound 19 leads to an increase in the lipidated and nonlipidated forms of LC3 similar to previous reports using PIK-III.
In vivo	The pharmacokinetic profile of analogue 19 is determined in C57BL/6 mice.?After oral administration at 10 mg/kg, the compound is rapidly absorbed and showed moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47).?Based on these PK parameters and the cellular activity, compound 19 constitutes a suitable candidate for in vivo studies.?Upon oral administration of compound 19 at 50 mg/kg twice a day (BID) for 7 days, LC3-II accumulates consistent with reduced autophagic capacity in time-dependent manner.?It inhibits autophagy in vivo.
Cell Research	Cell lines: U2OS cells.Concentrations: 0, 1, 5, 10 μM. Incubation Time: 24 h .Method: For inhibitor assay, cells are plated and the following day when cells had reached 90%, are treated with dimethyl sulfoxide (DMSO, vehicle) or the indicated concentration of PIK-III or Compound 19, both dissolved in DMSO. 24 hours later, cells are lysed in RIPA supplemented with 1% SDS and mini-EDTA protease inhibitors, homogenized by passage through a Qiashredder column and the protein is quantified by DC Lowry protein assay.
Animal Research	Animal Models: C57BL/6 Mice. Formulation: PG (20% v/v). Dosages: 10 mg/kg(p.o.) or 2 mg/kg(I.V.) .Administration: oral administration or I.V.

Synonyms	PIK-III analogue
Molecular Weight	391.47
Formula	C21H25N7O
CAS No.	1383716-46-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 78 mg/mL (199.25 mM)

References and Literature

1. Honda A , Harrington E , Cornella-Taracido I , et al. Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo[J]. ACS Medicinal Chemistry Letters, 2015, 7(1).

Citations

1. Yi W, Zhang J, Huang Y, et al.Ferritin-mediated mitochondrial iron homeostasis is essential for the survival of hematopoietic stem cells and leukemic stem cells.Leukemia.2024: 1-16.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Lung Cancer Compound Library Reprogramming Compound Library Antioxidant Compound Library Oxidation-Reduction Compound Library Glycolysis Compound Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library

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Keywords

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