Vps34-IN-1 free base

Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K.

For research use only. Not for human or veterinary use.

Target PI3K Autophagy

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Vps34-IN-1 structure

CAS No.: 1383716-33-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 420.00	BP-01880-250mg	In stock	Get quote
500 mg	USD 680.00	BP-01880-500mg	In stock	Get quote
1 g	USD 1,080.00	BP-01880-1g	In stock	Get quote
5 g	Inquire	BP-01880-5g	Inquire	Inquire

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Description

Vps34-IN-1 is a potent and selective inhibitor of class III Vps34 PI3K. Vps34-IN-1 inhibits phosphorylation of PtdIns by recombinant insect cell expressed Vps34-Vps15 complex with an IC50 of ~25 nM. Vps34-IN-1 can suppress SGK3 activation by reducing PtdIns(3)P levels via lowering phosphorylation of T-loop and hydrophobic motifs. Vps34-IN-1 modulates autophagy .

Biological activity

In Vitro Vps34-IN-1 does not significantly inhibit any of the lipid kinases including class I (p110α, p110β p110γ and p110δ) and all three members of the class II PI3Ks (PI3KC2α, PI3KC2β and PI3KC2γ) enzymes. Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) inhibits PtdIns(3)P levels at endosomes in a dose-dependent manner[1]. Vps34-IN-1 (0.01, 0.1, 1 μM; for 1 h) induces a dose-dependent reduction in SGK3 activity that is maximally lowered by ~60% at 1 μM and ~40% at 0.1 μM. The suppression of SGK3 activity is accompanied by a commensurate decrease in T-loop and hydrophobic motif phosphorylation[1]. Vps34-IN-1 (1, 2, 4 μM; 24 h) induces a dose-dependent inhibition of SGK3 phosphorylation.

Identifiers

SMILES: CC(C)(O)CNC1=NC=C(C(CC2CC2)=N1)C1=CC=NC(NC2=CC=NC(Cl)=C2)=N1
InChIKey: AWNXKZVIZARMME-UHFFFAOYSA-N

Specifications

MW (average): 425.9150
Formula: C₂₁H₂₄ClN₇O
CAS No.: 1383716-33-3
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Ruzica Bago, et al. Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase. Biochem J. 2014 Nov 1;463(3):413-27.

[2]. Fengchao Liu, et al. Prolonged inhibition of class I PI3K promotes liver cancer stem cell expansion by augmenting SGK3/GSK-3β/β-catenin signaling. J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.

[3]. Limpert AS, et al. Autophagy in Cancer: Regulation by Small Molecules. Trends Pharmacol Sci. 2018 Dec;39(12):1021-1032

Same target

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Same research area

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