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

Catalog No.S8456

Molecular Weight(MW): 391.47

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

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2mg	USD 147	In stock
5mg	USD 270	In stock
25mg	USD 870	In stock
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Description

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

Targets

VPS34 ^[1]
(Cell-free assay)

15 nM

In vitro

Compound 19 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^[1].

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^[1].

Protocol

Cell Research:^[1]	+ Expand 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. (Only for Reference)
Animal Research:^[1]	+ Expand 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. (Only for Reference)

Cell Research:^[1]

+ Expand

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.
(Only for Reference)

Animal Research:^[1]

+ Expand

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.
(Only for Reference)

References

[1] Honda A, et al. ACS Med Chem Lett. 2015, 7(1):72-6.

Solubility (25°C)

In vitro	DMSO	78 mg/mL (199.24 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download VPS34 inhibitor 1 (Compound 19, PIK-III analogue) SDF

Molecular Weight	391.47
Formula	C₂₁H₂₅N₇O
CAS No.	1383716-46-8
Storage	3 years -20°C powder
Synonyms	N/A

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