Identification of Small Molecules that Disrupt Signaling between ABL and Its Positive Regulator RIN1
Fig 5
Theaflavin-3,3’-digallate is a direct ABL kinase inhibitor.
0.5 nM purified ABL-eGFP was mixed with 2 μM CRK and 10 μM test compound and incubated in kinase buffer for 30 minutes at 30°C. Samples were analyzed by immunoblot using anti-phosphotyrosine. All the hits were screened, and a representative immunoblot is shown here. Test compounds were as follows: DMSO (ctrl), imatinib (IM), CID 16312764 (1), CID 467320 (2), CID 7457610 (3), CID 6084 (4), CID 4844281 (5), IUPAC 1-(4-phenylphenyl)-2-[4-(pyrimidin-2-yl)piperazin-1-yl]ethan-1-ol (6), CID 9291491 (7), CID 3991439 (8) and CID 16350799 (9).