Dyrk1A-IN-5

• CAT Number: I043559
• CAS Number: 1685235-41-9
• Molecular Formula: C16H9IN2O2
• Molecular Weight: 388.16
• Purity: ≥95%
• Synonyms: 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acid
• InChI: InChI=1S/C16H9IN2O2/c17-10-6-3-5-9-12-14(19-13(9)10)8-4-1-2-7-11(8)18-15(12)16(20)21/h1-7,19H,(H,20,21)
• InChIKey: SDRAETFVRBBLOB-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)C3=C(C4=C(N3)C(=CC=C4)I)C(=N2)C(=O)O

Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research[1].

Reference

[1]. Falke H, et al. 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A. J Med Chem. 2015 Apr 9;58(7):3131-43.
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