PI5P4Ks-IN-2

• CAT Number: I041152
• CAS Number: 2766854-03-7
• Molecular Formula: C22H23N5
• Molecular Weight: 357.45
• Purity: ≥95%
• Synonyms: 5-methyl-2-(2-propan-2-ylphenyl)-N-(pyridin-2-ylmethyl)pyrrolo[3,2-d]pyrimidin-4-amine
• InChI: InChI=1S/C22H23N5/c1-15(2)17-9-4-5-10-18(17)21-25-19-11-13-27(3)20(19)22(26-21)24-14-16-8-6-7-12-23-16/h4-13,15H,14H2,1-3H3,(H,24,25,26)
• InChIKey: XIEZMAUGHWKZDR-UHFFFAOYSA-N
• SMILES: CC(C)C1=CC=CC=C1C2=NC3=C(C(=N2)NCC4=CC=CC=N4)N(C=C3)C

PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC50 values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively[1].
PI5P4Ks-IN-2 (compound 40) (10 μM) shows selectivity against a panel of 140 protein kinases and 15 lipid kinases, and binds to PI5P4Kγ-WT (Ki=68 nM) or PI5P4Kβ (Ki >30,000 nM)[1].

Reference

[1]. Boffey HK, et al. Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode. J Med Chem. 2022 Feb 24;65(4):3359-3370.
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