ARUK2001607

ARUK2001607 is an inhibitor of phosphatidylinositol 5-phosphate 4-kinase gamma (PI5P4Kgamma, IC50 = 0.079 µM for PI5P4Kgamma+, a construct with mutations conferring increased functional activity). It selectively binds to PI5P4Kgamma (Kd = 7.1 nM) over 22 other lipid kinases but does bind to phosphatidylinositol 4-phosphate 5-kinase type-1 gamma (PIP5K1C, Kd = 230 nM). ARUK2001607 is selective for PI5P4Kgamma over PI5P4Kalpha and PI5P4Kbeta (IC50s = >15.8 and >25.1 µM, respectively). It is also selective for PI5P4Kgamma over 138 other kinases in a kinase panel and a variety of receptors, enzymes, and ion channels in a safety panel at 10 µM but does inhibit Aurora B kinase and CDC-like kinase 2 (CLK2) by 31 and 37% and dopamine uptake by 59% at 10 µM.Formal Name: 6-methyl-N-[4-(methylsulfonyl)phenyl]-thieno[2,3-d]pyrimidin-4-amine. CAS Number: 2924824-56-4. Molecular Formula: C14H13N3O2S2. Formula Weight: 319.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml. SMILES: O=S(C1=CC=C(NC2=C3C=C(C)SC3=NC=N2)C=C1)(C)=O. InChi Code: InChI=1S/C14H13N3O2S2/c1-9-7-12-13(15-8-16-14(12)20-9)17-10-3-5-11(6-4-10)21(2,18)19/h3-8H,1-2H3,(H,15,16,17). InChi Key: QVQHWPLHUNEREE-UHFFFAOYSA-N.