A PI5P4Kγ inhibitor
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ARUK2001607

Item No. 41527

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-methyl-N-[4-(methylsulfonyl)phenyl]-thieno[2,3-d]pyrimidin-4-amine
CAS Number
2924824-56-4
Molecular Formula
C14H13N3O2S2
Formula Weight
319.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=S(C1=CC=C(NC2=C3C=C(C)SC3=NC=N2)C=C1)(C)=O
InChi Code
InChI=1S/C14H13N3O2S2/c1-9-7-12-13(15-8-16-14(12)20-9)17-10-3-5-11(6-4-10)21(2,18)19/h3-8H,1-2H3,(H,15,16,17)
InChi Key
QVQHWPLHUNEREE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $196

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    25 mg

    $382

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    50 mg

    $600

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    Product Description

    ARUK2001607 is an inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ; IC50 = 0.079 µM for PI5P4Kγ+, a construct with mutations conferring increased functional activity).1 It selectively binds to PI5P4Kγ (Kd = 7.1 nM) over 22 other lipid kinases but does bind to phosphatidylinositol 4-phosphate 5-kinase type-1 γ (PIP5K1C; Kd = 230 nM). ARUK2001607 is selective for PI5P4Kγ over PI5P4Kα and PI5P4Kβ (IC50s = >15.8 and >25.1 µM, respectively). It is also selective for PI5P4Kγ over 138 other kinases in a kinase panel and a variety of receptors, enzymes, and ion channels in a safety panel at 10 µM but does inhibit Aurora B kinase and CDC-like kinase 2 (CLK2) by 31 and 37% and dopamine uptake by 59% at 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rooney, T.P.C., Aldred, G.G., Boffey, H.K., et al. The identification of potent, selective, and brain penetrant PI5P4Kγ inhibitors as in vivo-ready tool molecules. J. Med. Chem. 66(1), 804-821 (2023).