A DYRK1A inhibitor
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DYRK1A Inhibitor Compound 11

Item No. 41715

Technical Information
Formal Name
N,N-dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine
CAS Number
2814486-79-6
Synonyms
  • Dual-specificity Tyrosine Phosphorylation-regulated Kinase 1A Inhibitor Compound 11
  • DYRK1-IN-1
  • DYRK1 Inhibitor 1
Molecular Formula
C12H12N6
Formula Weight
Purity
≥98%
A solid
DMSO: Slightly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CN(C)C1=NC=CC(C2=C3N(N=CC=C3)N=C2)=N1
InChi Code
InChI=1S/C12H12N6/c1-17(2)12-13-7-5-10(16-12)9-8-15-18-11(9)4-3-6-14-18/h3-8H,1-2H3
InChi Key
IFLBFWBMAWIBBZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    DYRK1A inhibitor compound 11 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A; IC50 = 0.4 nM).1 It is selective for DYRK1A over DYRK2, CDC-like kinase 1 (Clk1), Clk2, Clk3, cyclin-dependent kinase 2 (Cdk2), and glycogen synthase kinase 3β (GSK3β; IC50s = 19, 7.1, 9.4, 54, 100, and 94 nM, respectively) but does inhibit DYRK1B (IC50 = 2.7 nM). DYRK1A inhibitor compound 11 inhibits DYRK1A-induced increases in tau phosphorylation in a cell-based assay (IC50 = 590 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Henderson, S.H., Sorrell, F., Bennett, J., et alDiscovery and characterization of selective and ligand-efficient DYRK inhibitors. J. Med. Chem. 64(15), 11709-11728 (2021).