A selective inhibitor of Vps34
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Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

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PIK-III

Item No. 17002

Technical Information
Formal Name
4'-(cyclopropylmethyl)-N2-4-pyridinyl-[4,5'-bipyrimidine]-2,2'-diamine
CAS Number
1383716-40-2
Synonyms
  • Vacuolar Protein Sorting 34 Inhibitor 2
  • Vps34-IN2
  • Vps34 Inhibitor 2
Molecular Formula
C17H17N7
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 0.14 mg/mlPBS (pH 7.2): slightly
λmax
284 nm
SMILES
NC(N=C1)=NC(CC2CC2)=C1C3=CC=NC(NC4=CC=NC=C4)=N3
InChi Code
InChI=1S/C17H17N7/c18-16-21-10-13(15(23-16)9-11-1-2-11)14-5-8-20-17(24-14)22-12-3-6-19-7-4-12/h3-8,10-11H,1-2,9H2,(H2,18,21,23)(H,19,20,22,24)
InChi Key
XXSDLQLNIVFIJI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PIK-III is an inhibitor of the type 3 phosphatidylinositol 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34) that binds a unique hydrophobic pocket (IC50 = 18 nM).1 It is selective for Vps34 over related PI3K isoforms, PI4Kβ, and mTOR. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, leading to stabilization of autophagy substrates.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dowdle, W.E., Nyfeler, B., Nagel, J., et alSelective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat. Cell Biol. 16(11), 1069-1079 (2014).

    Product Citations

    Young, A.N., Herrera, D., Huntsman, A.C., et alPhyllanthusmin derivatives induce apoptosis and reduce tumor burden in high-grade serous ovarian cancer by late-stage autophagy inhibition. Mol. Cancer Ther. 17(10), 2123-2135 (2018).