An AAK1 and BMP2K inhibitor
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LP-935509

Item No. 37283

Technical Information
Formal Name
4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-1-piperazinecarboxylic acid, 1-methylethyl ester
CAS Number
1454555-29-3
Molecular Formula
C20H24N6O3
Formula Weight
Purity
≥98%
A solid
λmax
268, 308, 321 nm
SMILES
O=C(N1CCN(CC1)C2=NC3=C(C4=C(OC)N=CC=C4)C=NN3C=C2)OC(C)C
InChi Code
InChI=1S/C20H24N6O3/c1-14(2)29-20(27)25-11-9-24(10-12-25)17-6-8-26-18(23-17)16(13-22-26)15-5-4-7-21-19(15)28-3/h4-8,13-14H,9-12H2,1-3H3
InChi Key
GOOYSJIWTIHOGW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LP-935509 is an inhibitor of AP2-associated protein kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K; IC50s = 3.3 and 14 nM, respectively).1 It is selective for AAK1 and BMP2K over μ- and κ-opioid, as well as α2A- and α2C-adrenergic, receptors (IC50s = >30 µM for all), α1 and α2 subunit-containing GABAA receptors (IC50s = 12 µM for both), and cyclin G-associated kinase (GAK; IC50 = 0.32 µM). LP-935509 (1 µM) reduces phosphorylation of the synaptic vesicle regulator AP2 complex subunit Μu-1 (AP2M1) in SH-SY5Y neuroblastoma cells.2 It reduces the number of formalin-induced flinches in mice when administered at doses of 10, 30, and 60 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kostich, W., Hamman, B.D., Li, Y.-W., et alInhibition of AAK1 kinase as a novel therapeutic approach to treat neuropathic pain. J. Pharmacol. Exp. Ther. 358(3), 371-386 (2016).

    2. Liu, Q., Bautista-Gomez, J., Higgins, D.A., et alDysregulation ofthe AP2M1 phosphorylation cycle by LRRK2 impairs endocytosis and leads to dopaminergic neurodegeneration. Sci. Signal. 14(693), eabg3555 (2021).