An inhibitor of PI5P4K
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NIH 12848

Item No. 26035

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-thienylmethyl)-2-[2-(trifluoromethyl)phenyl]-4-quinazolinamine
CAS Number
959551-10-1
Molecular Formula
C20H14F3N3S
Formula Weight
385.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 25 mg/mL
λmax
231, 317 nm
SMILES
FC(C(C=CC=C1)=C1C2=NC3=CC=CC=C3C(NCC4=CC=CS4)=N2)(F)F
InChi Code
InChI=1S/C20H14F3N3S/c21-20(22,23)16-9-3-1-7-14(16)19-25-17-10-4-2-8-15(17)18(26-19)24-12-13-6-5-11-27-13/h1-11H,12H2,(H,24,25,26)
InChi Key
QBDAEJRHUCSSPR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $178

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    25 mg

    $389

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    Product Description

    NIH 12848 is an inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ; IC50 = ~1 µM).1 It is selective for PI5P4Kγ over PI5P4Kα and PI5P4Kβ (IC50s = >100 µM). NIH 12848 inhibits translocation of the Na+/K+-ATPase to the plasma membrane in mouse principal kidney cortical collecting duct (mpkCCD) cells. NIH 12848 is also an inhibitor of USP1/UAF complex deubiquitinase activity (IC50 = 7.9 µM).2 It increases accumulation of monoubiquitinated proliferating cell nuclear antigen (PCNA) in H1299 non-small cell lung cancer (NSCLC) cells when used at a concentration of 20 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clarke, J.H., Giudici, M.L., Burke, J.E., et al. The function of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) explored using a specific inhibitor that targets the PI5P-binding site. Biochem. J. 466(2), 359-367 (2015).

    2. Dexheimer, T.S., Rosenthal, A.S., Luci, D.K., et al. Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer. J. Med. Chem. 57(19), 8099-8110 (2014).