A potent and selective inhibitor of VPS34
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VPS34-IN-1

Item No. 17392

Technical Information
Formal Name
1-[[2-[(2-chloro-4-pyridinyl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino]-2-methyl-2-propanol
CAS Number
1383716-33-3
Synonyms
  • Vacuolar Protein Sorting 34 Inhibitor 1
  • VPS34 Inhibitor 1
Molecular Formula
C21H24ClN7O
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: 35 mg/ml
λmax
286 nm
SMILES
OC(C)(C)CNC1=NC(CC2CC2)=C(C3=CC=NC(NC4=CC=NC(Cl)=C4)=N3)C=N1
InChi Code
InChI=1S/C21H24ClN7O/c1-21(2,30)12-26-19-25-11-15(17(29-19)9-13-3-4-13)16-6-8-24-20(28-16)27-14-5-7-23-18(22)10-14/h5-8,10-11,13,30H,3-4,9,12H2,1-2H3,(H,25,26,29)(H,23,24,27,28)
InChi Key
AWNXKZVIZARMME-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VPS34-IN-1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34; IC50 = 25 nM in vitro).1 It does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. VPS34-IN-1 dose-dependently inhibits generation of PtdIns-(3)-p, which is essential to the formation and trafficking of endsomes and autophagosomes, without affecting the ability of class I PI3K to regulate Akt. It induces a rapid and pronounced loss of phosphorylation on serum- and glucocorticoid-regulated kinase 3.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bago, R., Malik, N., Munson, M.J., et alCharacterization 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. 463(3), 413-427 (2014).

    Product Citations

    Liu, F., Zuo, X., Liu, Y., et alSuppression of membranous LRP5 recyling, Wnt/β-catenin signaling, and colon carcinogenesis by 15-LOX-1 peroxidation of linoleic acid in PI3P. Cell Rep. 32(7), 108049 (2020).