Compound 1

Chemical libraries for HTS were acquired from various sources. An additional batch of compound 1 was purchased from ChemBridge Corp. (San Diego, CA) for revalidation. All other chemicals were purchased from Sigma-Aldrich (St. Louis, MO) unless stated otherwise. Restriction DNA endonucleases and DNA ligases were purchased from New England Biolabs (Beverly, MA). SYBR green I stain was purchased from Life Technologies (Carlsbad, CA). The AlphaScreen assay kit was purchased from PerkinElmer (Waltham, MA). Taq DNA polymerases for PCR, the PCR purification kit, and the Plasmid Miniprep kit were purchased from Qiagen (Valencia, CA). COS7 and HeLa cells were obtained from American Type Culture Collection (Manassas, VA) and cultured in Dulbecco’s Modified Eagle Medium containing 10% FBS. All cells were maintained in an incubator at 37°C in a humidified atmosphere of 5% carbon dioxide.

Compound 1 was purchased from ChemBridge and compounds 2, 3, and 4 were synthesized by ENAMINE Ltd. The products were isolated and purified until it was more than 95% pure as determined by LC/MS and ¹H NMR. Full details in the Supporting Information.